NF-κB

NF-κB抑制剂选择性比较

NF-κB信号通路图

NF-κB信号通路图

NF-κB产品

  • 所有产品(117)
  • NF-κB抑制剂 (108)
  • NF-κB激活剂 (2)
  • NF-κB调节剂 (5)
目录号 产品名 产品描述 文献引用 实验数据
S1013 Bortezomib (PS-341) Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239)是有效的蛋白酶抑制剂,Ki为0.6 nM。它对肿瘤细胞表现出良好的选择性。Bortezomib (PS-341) 可抑制 NF-κB 并诱导 ERK 的磷酸化从而抑制cathepsin B并在卵巢癌和其他固体肿瘤中抑制自噬的催化过程。
Mol Cell, 2022, S1097-2765(22)00433-6
Sci Immunol, 2022, 7(68):eabi6763
Sci Adv, 2022, 8(4):eabi7711
S2824 TPCA-1 TPCA-1 (GW683965)是一种IKK-2抑制剂,无细胞试验中IC50为17.9 nM,抑制NF-κB通路,比作用于IKK-1选择性高22倍。TPCA-1 也是 STAT3 的抑制剂并可促进凋亡。
Nat Cell Biol, 2022, 24(5):766-782
Sci Adv, 2022, 8(12):eabh4050
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
S4902 QNZ (EVP4593) QNZ (EVP4593)有效抑制NF-κB激活和TNF-α产生,在Jurkat T细胞中IC50分别为11 nM和7 nM。
Cell Death Differ, 2022, 10.1038/s41418-022-00940-1
Cell Death Dis, 2022, 13(5):495
Cell Death Dis, 2022, 13(4):420
S8078 Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) 是一种IKK抑制剂,具有强的促凋亡和抗炎活性。同时还是有效的Nrf2激活剂和NF-κB抑制剂。Bardoxolone Methyl 可抑制铁死亡。Bardoxolone Methyl 在癌细胞中可诱导凋亡和自噬。
Drug Des Devel Ther, 2021, 15:21-35
Cancers (Basel), 2020, 12(6):E1645
Antioxidants (Basel), 2020, 9(1)
S1623 Acetylcysteine (N-acetylcysteine) Acetylcysteine (N-acetyl-l-cysteine, NAC)是ROS抑制剂,拮抗多种蛋白酶体抑制剂的活性。它还是肿瘤坏死因子TNF的抑制剂,主要用作祛痰剂,可通过维持或恢复肝脏中谷胱甘肽的浓度来处理扑热息痛(对乙酰氨基酚过量)。Acetylcysteine(N-acetyl-l-cysteine) 通过抑制IκB kinases抑制TNF诱导的NF-κB活化。Acetylcysteine(N-acetyl-l-cysteine) 通过线粒体依赖性途径诱导凋亡并抑制铁死亡和病毒复制。现配现用
EMBO Mol Med, 2022, 14(2):e14903
J Exp Clin Cancer Res, 2022, 41(1):41
Environ Sci Technol, 2022, 10.1021/acs.est.2c00585
E2661New Chitosan oligosaccharide Chitosan oligosaccharide (COS)是β-(1➔4)连接的d-氨基葡萄糖的低聚物,其作用涉及几个重要的途径的调节,包括抑制核因子κB (nuclear factor kappa B, NF-κB)丝裂原活化蛋白激酶(mitogen-activated protein kinases, MAPK),以及活化AMP -活化蛋白激酶(AMP-activated protein kinase, AMPK)
E0796New NF-κB-IN-1 NF-κB-IN-1是一种有效的NF-κB信号通路抑制剂,通过直接抑制抑制性κB激酶(inhibitory κB kinase, IKK)起作用。
E0783New SM-7368 SM-7368是一种有效的NF-κB抑制剂,可靶向MAPK p38激活的下游,也能抑制TNF-α诱导的MMP-9上调。
E0526New sappanone A Sappanone A是从豆科苏木心材中分离得到的一种异黄酮类化合物,通过p38 MAPK通路激活Nrf2,诱导HO-1表达,并通过抑制RelA/p65在Ser536位点的磷酸化来抑制脂多糖诱导的NF-κB的激活,发挥其抗炎作用。
S8989New Xanthatin Xanthatin是一种从中药苍耳(Xanthium strumarium)叶子中分离得到的倍半萜内酯,可抑制核因子kappa-B (nuclear factor kappa-B, NF-κB)、丝裂原活化蛋白激酶(mitogen-activated protein kinase, MAPK)以及信号转导和转录激活因子(signal transducer and activator of transcription, STATs)信号通路
E0212New Cornuside Cornuside 是一种从 Cornus officinalis SIEB. et ZUCC 果实中分离出来的双环烯醚萜苷化合物。Cornuside 通过抑制 RAW 264.7 巨噬细胞中的 NF-κB 活化来抑制脂多糖诱导的炎症介质。Cornuside 减弱大鼠皮质神经元的细胞凋亡。
E0022New Ophiopogonin D Ophiopogonin D (OJV-VI, Deacetylophiopogonin C) 是一种从中草药麦冬中分离得到的甾体糖苷,具有抗肿瘤作用。Ophiopogonin D 可通过调节 ITGB1/FAK/Src/AKT/β-catenin/MMP-9 信号轴抑制TGF-β1介导的MDA-MB-231细胞转移行为。Ophiopogonin D 还通过抑制小鼠肺上皮细胞中的 AMPK/NF-κB 通路来减轻 PM2.5 诱导的炎症。
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow)是流行的印度香料姜黄的主要姜黄色素,属于姜科(Zingiberaceae)。它是p300 histone acetylatransferase(IC50~25 μM)和Histone deacetylase (HDAC)的抑制剂,能够激活Nrf2 pathway并抑制NF-κB的激活。Curcumin 可诱导线粒体自噬、细胞自噬、凋亡和细胞周期阻滞,并具有抗肿瘤的活性。Curcumin 可通过减少铁死亡介导的细胞死亡来减少横纹肌溶解相关的肾衰竭。Curcumin 对各种人类病原体(如流感病毒,丙型肝炎病毒,HIV等)具有抗感染特性。
Phytother Res, 2022, 36(3):1326-1337
Dis Markers, 2022, 2022:3129781
Adv Sci (Weinh), 2021, e2103360
S4073 Sodium 4-Aminosalicylate Sodium 4-Aminosalicylate是一种用于治疗肺结核的抗生素,通过NF-κB的抑制和自由基清除起作用。
In Vitro Cell Dev Biol Anim, 2019, 55(5):368-375
PLoS One, 2016, 11(3):e0149754
S7351 JSH-23 JSH-23是一种NF-κB转录活性抑制剂,在RAW 264.7细胞系中IC50为7.1 μM。
Nat Cell Biol, 2022, 24(5):766-782
Int J Biol Sci, 2022, 18(5):2132-2145
Int J Mol Sci, 2022, 23(6)3280
S1576 Sulfasalazine (NSC 667219) Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) 是一种磺胺剂,是Mesalazine的衍生物,主要用作抗炎剂。Sulfasalazine 是一种有效的、特异性的 nuclear factor kappa B (NF-κB)TGF-βCOX-2 的抑制剂。Sulfasalazine 可诱导铁死亡、凋亡和自噬。
Cell Mol Life Sci, 2022, 79(5):228
Front Bioeng Biotechnol, 2022, 10:855755
Cell Metab, 2021, S1550-4131(21)00233-3
S7414 Caffeic Acid Phenethyl Ester Caffeic acid phenethyl ester (CAPE, Phenylethyl Caffeate)是强效的特异性NF-κB活化抑制剂,也能够表现出抗氧化、免疫调节和抗炎活动。
Oncogene, 2022, 10.1038/s41388-022-02253-6
Cancers (Basel), 2022, 14(2)274
J Exp Clin Cancer Res, 2021, 40(1):87
S3137 Sodium salicylate Sodium salicylate用来作为镇痛药和退烧药,是一种非甾类消炎药 (NSAID), 在癌细胞中可以诱导细胞凋亡和坏死。在转染的T细胞中,Sodium salicylate可以抑制 NF-kappa B的激活, 也可以抑制依赖NF-kappa B 的转录,包括Ig kappa 增强子 以及 人类免疫缺陷病毒 (HIV) 长末端重复序列(LTR)。
Theranostics, 2020, 10(17):7747-7757
S3939 4'-Methoxyresveratrol 4-Methoxyresveratrol is a stibenoid found in the Chinese herb Gnetum cleistostachyum. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation.
S4798 Benfotiamine Benfotiamine (S-Benzoylthiamine O-monophosphate) is a synthetic S-acyl derivative of thiamine (vitamin B1) and has been investigated for the treatment and prevention of Diabetic Nephropathy and Diabetes Mellitus, Type 2. Benfotiamine suppresses oxidative stress-induced NF-κB activation and prevents the bacterial endotoxin-induced inflammation.
J Mol Model, 2022, 28(6):153
S0002 IAXO-102 IAXO-102 是一种靶向MD-2和CD14共同受体的 TLR4 的拮抗剂。IAXO-102 可抑制 MAPK 和p65 NF-κB 磷酸化,并下调TLR4依赖性促炎蛋白的表达。IAXO-102 可抑制实验性腹主动脉瘤 (AAA) 的发展。
S6899 Licochalcone D Licochalcone D (Lico D, LCD, LD) 是一种从中草药甘草 Glycyrrhiza inflata 中分离出的类黄酮,具有抗氧化、抗炎和抗癌的特性。Licochalcone D 可抑制LPS信号通路中NF-κB p65的磷酸化。Licochalcone D 可抑制 JAK2EGFRMet (c-Met) 活性,并诱导ROS依赖性的凋亡。Licochalcone D 还可诱导 caspases 的活化和 poly (ADP-ribose) polymerase (PARP) 的裂解。
S8279 Shikonin (C.I. 75535) Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844)是一种 Pyruvate kinase M2 (PKM2) 有效的、特异的抑制剂。它是紫草的主要成分,紫草是一种中草药,具有多种生物活性。在细胞荧光淬灭试验中,Shikonin也是TMEM16A氯离子通道的抑制剂。Shikonin 通过抑制 tumor necrosis factor-α (TNF-α) 发挥抗炎作用,并可通过抑制 proteasome 来阻止 nuclear factor-κB (NF-κB) 信号途径的激活。
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Mil Med Res, 2022, 9(1):22
S0911 Hypaphorine Hypaphorine 大量存在于王不留行vaccaria semen中,通过抑制 ERK 或/和NFκB信号通路来抵消炎症。
S7672 Omaveloxolone (RTA-408) Omaveloxolone (RTA-408)是一种合成的三萜类化合物,其激活细胞保护转录因子 Nrf2 并抑制 NF-κB 信号。Phase 2。
Brain Behav, 2021, 11(1):e01918
Cancers (Basel), 2020, 12(9)E2668
Int J Neurosci, 2020, 7:1-16
S3223 L-Quebrachitol L-Quebrachitol (L-QCT) 是可从许多植物中分离出来的天然产物,促进增殖和细胞DNA合成。L-Quebrachitol 可上调 bone morphogenetic protein-2 (BMP-2)runt-related transcription factor-2 (Runx2)mitogen-activated protein kinase (MAPK) 相关调控基因和 Wnt/β-catenin 信号通路,同时下调 nuclear factor-κB(NF-κB) 配体 (RANKL) 受体激活剂的mRNA水平。
S3998 (+)-α-Lipoic acid (+)-α-Lipoic acid ((R)-(+)-α-Lipoic acid, α-Lipoic acid, Alpha-Lipoic acid)是thioctic acid的生理形式之一,是一种强效的抗氧化剂,可减轻糖尿病神经性症状。它比其外消旋体具有更优越的抗氧化性。R(+)-α-lipoic acid 是线粒体酶复合物的必要辅助因子。R(+)-α-lipoic acid 抑制 NF-κB 依赖性HIV-1 LTR 活化。
S0507 CBL0137 CBL0137 (Curaxin-137)是一种 histone chaperone FACT (facilitates chromatin transcription) 的抑制剂,可同时抑制 NF-κB 并激活 p53,对应的EC50值分别为0.47 μM和0.37 μM。
Cancer Lett, 2021, 520:201-212
Cancer Lett, 2021, 499:232-242
PLoS One, 2021, 16(6):e0252504
S5144 Neferine Neferine ((R)-1,2-Dimethoxyaporphine) 是 Nelumbo nucifera 的天然成分,具有抗肿瘤功效。Neferine 可诱导肾癌细胞凋亡。Neferine 通过激活肌肉细胞中的 Akt/mTOR 通路和 Nrf2 来防止自噬。Neferine 可抑制 NF-κB 的激活。Neferine具有多种治疗作用,例如抗糖尿病,抗衰老,抗微生物,抗血栓形成,抗心律不齐,抗炎甚至抗HIV。
Bone Res, 2022, 10(1):27
Oncol Rep, 2020, 44(3):1116-1126
S9208 Ginsenoside Rb3 Ginsenoside Rb3 是从人参中提取的天然产物,在心血管疾病包括心肌的缺血/再灌注(I/R)损伤中起着重要作用。在人肾293T细胞中检测了Ginsenoside Rb3(0.1-10 μM)对肿瘤坏死因子TNF-α诱导的 nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) 荧光素酶报告基因的抑制作用,IC50值为8.2 μM。在用10 ng/mL TNF-α处理后的HepG2细胞中,Ginsenoside Rb3 还以剂量依赖性的方式抑制 cyclooxygenase-2 (COX-2)inducible nitric oxide synthase (iNOS) 信使mRNA的诱导诱导表达。
S0923 Isoliquiritin apioside Isoliquiritin apioside (ISLA, ILA) 是一种分离自 Glycyrrhizae radix rhizome (GR) 的成分,可显著地降低PMA诱导的 matrix metalloproteinase (MMP) 的活性增加并抑制了PMA-诱导 mitogen-activated protein kinase (MAPK)NF-κB 的活化。Isoliquiritin apioside 在恶性癌细胞和EC中具有抗转移和抗血管生成的能力,并且没有细胞毒性。
S8961 Alobresib (GS-5829) Alobresib (GS-5829) 是一种新型的 BET 抑制剂,是一种针对复发/耐药的USC过表达c-Myc的高效治疗剂。Alobresib (GS-5829) 可抑制CLL细胞增殖并通过解除如 BLKAKTERK1/2MYC等关键信号通路的管制来诱导白血病细胞凋亡apoptosis。Alobresib (GS-5829) 还可抑制 NF-κB 的信号传导。
S3633 Pyrrolidinedithiocarbamate ammonium Pyrrolidinedithiocarbamate ammonium (Ammonium pyrrolidine dithiocarbamate, APDC, PDTC, Pyrrolidine dithiocarbamic acid ammonium salt)是NF-κB的有效抑制剂,抑制IκB磷酸化、阻止NF-κB易位入核并减少下游细胞因子的表达。
Signal Transduct Target Ther, 2022, 7(1):46
Cell Mol Life Sci, 2022, 79(2):86
Theranostics, 2022, 12(2):910-928
S0931 Jaceosidin Jaceosidin 是一种从Artemisia vestita中分离出来的类黄酮,在许多癌细胞中均具有抗肿瘤和抗增殖的活性。Jaceosidin 诱导凋亡,激活 Bax 并下调 Mcl-1c-FLIP 表达。Jaceosidin 可抑制 COX-2 的表达和 NF-κB 的激活。
S3901 Astragaloside IV Astragaloside IV (AST-IV, AS-IV) is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. AS-IV suppresses activation of p-Akt, p-mTOR, p-NF-κB and p-Erk1/2.
Naunyn Schmiedebergs Arch Pharmacol, 2020, 10.1007/s00210-020-02022-w
S3231 UCB-9260 UCB-9260 是一种口服活性抑制剂,可通过稳定三聚体的不对称形式来抑制 TNF 信号传导。 UCB-9260 与TNF结合的Kd值为13 nM。UCB-9260 还抑制TNF刺激后NF-κB,对应的IC50值为202 nM。
S3816 Dehydroevodiamine Dehydroevodiamine (DHED), a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.
S9244 8-O-acetyl shanzhiside methyl ester 8-O-acetyl shanzhiside methyl ester (Barlerin, ND01), isolated from the leaves of Lamiophlomis rotata Kudo, promotes angiogenesis, which leads to the improvement of functional outcome after stroke.8-O-Acetyl shanzhiside methyl ester can inhibts NF-κB.
S3384 (E/Z)-IT-603 (E/Z)-IT-603 是 E-IT-603 和 Z-IT-603的混合物。IT-603 是一种NF-κB 家族成员 c-Rel 抑制剂,在电泳迁移率变化试验 (EMSA) 中的 IC50 为 3 μM。
S5640 Ethyl caffeate Ethyl caffeate, a naturally occurring compound found in Bidens pilosa, suppresses NF-kappaB activation and its downstream inflammatory mediators, iNOS, COX-2 and PGE2 in vitro.
S0781 IQ 3 IQ 3 是一种特定的 c-Jun N-terminal kinase (JNK) 的抑制剂,对JNK3、JNK1和JNK2的Kd值分别为66 nM、240 nM和290 nM。IQ 3 可抑制TPS1-Blue细胞中LPS诱导的 NF-κB/AP1 的转录活性,IC50值为1.4 μM。IQ 3 还可以在体外实验中抑制 TNF-αIL-6 的产生。
S2261 Andrographolide Andrographolide是一种Labdane类二萜,是药用植物Andrographis paniculata的主要生物活性成分
Oxid Med Cell Longev, 2021, 2021:5577634
Int J Oncol, 2020, 56(6):1417-1428
Eur J Pharmacol, 2020, 873:172981
S2382 Evodiamine Evodiamine (Isoevodiamine)是Evodiae Fructus中提取的一种生物碱。它能通过抑制IkB kinase活性抑制NF-kB的激活。
Chem Biol Interact, 2021, 351:109756
Anticancer Drugs, 2021, 32(3):314-322
J Exp Clin Cancer Res, 2020, 39(1):249
S5771 Sulforaphane Sulforaphane 是一种天然存在的异硫氰酸盐,存在于十字花科蔬菜如西兰花、卷心菜、羽衣甘蓝。它是 Nrf2 的诱导物。Sulforaphane 也是 histone deacetylase (HDAC)NF-κB 的抑制剂。Sulforaphane 可增加 heme oxygenase-1 (HO-1),并降低 reactive oxygen species (ROS) 的水平。Sulforaphane 诱导细胞周期停滞和凋亡。
Elife, 2022, 11e67368
Cell Death Discov, 2021, 7(1):375
Cell Commun Signal, 2021, 19(1):35
S4937 4'-Hydroxychalcone 4'-Hydroxychalcone (P-Cinnamoylphenol),存在于草药、香料和茶叶中,是一种刺甘草查尔酮。它具有多种生物活性,能够抑制TNF-α诱导的NF-κB通路激活、并激活BMP信号通路。
S9295 Dauricine Dauricine, a plant metabolite isolated from the Asian vine Menispermum dauricum, plays a variety of biological roles in the human body, from inhibiting cancer cell growth to blocking cardiac transmembrane Na+, K+, and Ca2+ ion currents.Dauricine induces apoptosis, inhibits proliferation and invasion through inhibiting NF‐κB signaling pathway in colon cancer cells.
S5343 Vanillic acid Vanillic acid (4-hydroxy-3-methoxybenzoic acid) is a flavoring agent which is also an intermediate in the production of vanillin from ferulic acid. Vanillic acid inhibits NF-κB activation. Anti-inflammatory, antibacterial, and chemopreventive effects.
S2290 Dihydroartemisinin (DHA) Dihydroartemisinin (DHA, Dihydroqinghaosu, β-Dihydroartemisinin, Artenimol)是一种Artemisinin 的半合成衍生物,从传统中药Artemisia annua分离而来的。Dihydroartemisinin 可通过抑制 NF-κB 激活来诱导自噬和凋亡。
Front Pharmacol, 2022, 13:884881
Front Endocrinol (Lausanne), 2022, 13:891922
Nat Immunol, 2021, 10.1038/s41590-021-00967-5
S9193 Aristolochic acid A Aristolochic acid A (Aristolochic Acid I, Aristolochin, Aristolochine, TR 1736)是一种致癌、致突变和具有肾毒性的试剂,来源于马兜铃科的开花植物。Aristolochic acid A 可显著降低 activator protein 1 (AP-1)nuclear factor-κB (NF-κB) 的活性。
Mol Ther Nucleic Acids, 2020, 6;19:1276-1289
Am J Physiol Renal Physiol, 2020, 319(6):F1003-F1014
S7428 Rocaglamide Rocaglamide (Roc-A) 是从Aglaia物种中分离出来的一种有效的 heat shock factor 1 (HSF1) 活化的抑制剂,对HSF1的IC50值约为50 nM。Rocaglamide 可抑制翻译起始因子 eIF4A 的功能。Rocaglamide 还抑制 NF-κB 的活性。Rocaglamide 具有抗肿瘤活性。
S7445 E3330 E3330 (APX-3330)是一种有效的选择性APE1(Ref-1)抑制剂,其抑制 NF-κB DNA-结合活性。
Cell Death Dis, 2022, 13(2):124
Cancer Research on Prevention and Treatment, 2020, (7): 492-497
S2313 Indole-3-carbinol Indole-3-carbinol是通过降解硫代葡萄糖酸盐芸苔葡萄糖硫苷而来的,广泛存在于十字花科蔬菜中。它能够抑制NF-κBIκBα激酶的激活。
Am J Cancer Res, 2021, 11(10):4994-5005
J Med Virol, 2019, 91(8):1440-1447
S3931 Ginsenoside Rd Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S9040 Maslinic acid Maslinic Acid (Crategolic Acid, 2α-Hydroxyoleanoic Acid), a Natural Triterpene, exerts a wide range of biological activities, i.e. antitumor, antidiabetic, antioxidant, cardioprotective, neuroprotective, antiparasitic and growth-stimulating. MA significantly suppresses the DNA-binding activity of NF-κB p65 in LPS-induced RAW 264.7 cells.
S8587 Withaferin A Withaferin A (WA, WFA)可通过对硫代烷基化敏感的氧化还原机制阻止肿瘤坏死因子诱导的IκB激酶β的激活,从而有效地抑制 NF-κB 激活。Withaferin A 可与中间丝状体蛋白(IF) vimentin 结合,并具有抗肿瘤和抗血管生成活性。Withaferin A 是一种从 Withania somnifera 分离的甾体内酯。
Antioxidants (Basel), 2021, 10(7)1063
Mol Cell Biol, 2021, MCB0046721
bioRxiv, 2021, 10.1101/2021.02.04.429815
S7273 SC75741 SC75741 是强效的NF-κB抑制剂,其EC50为200 nM。SC75741 可有效地阻断流感病毒的传播。
Front Immunol, 2022, 13:839460
Int J Mol Sci, 2022, 23(6)3280
Microbiol Spectr, 2022, e0188121
S3760 Stachydrine hydrochloride Stachydrine is isolated from seed husk and the pulp of the fruit of C. Leonurus, and many other Asian plants and fruits. It has potent anti-metastatic activity and cardioprotective effects. Stachydrine hydrochloride is the major active constituent of Herba Leonuri, which is a potential therapy for cardiovascular diseases. Stachydrine can inhibit the NF-κB signal pathway. Anti-hypertrophic activities.
Pharm Biol, 2022, 60(1):700-707
S5899 (R)-(-)-Ibuprofen (R)-(-)-Ibuprofen ((R)-Ibuprofen) 可抑制T细胞刺激下 NF-κB 的激活,其IC50值为121.8 μM,且具有抗炎和镇痛作用。
S3293 Gardenoside Gardenoside 是一种从Gardenia栀子属果实中提取的天然化合物,具有保肝作用。Gardenoside 可抑制 TNF-αIL-1βIL-6NFκB 的活化。Gardenoside 还对游离脂肪酸(FFA)诱导的细胞脂肪变性具有抑制作用。Gardenoside 可通过调节 P2X3P2X7 受体来减轻慢性压迫性损伤大鼠的疼痛。
S3770 Sodium Aescinate Sodium Aescinate (SA, Escin Sodium Salt) is a widely-applied triterpene saponin product derived from horse chestnut seeds, possessing vasoactive and organ-protective activities with oral or injection administration in the clinic. Sodium aescinate is a triterpene saponin derived from Aesculus hippocastanum seeds, with anti-inflammatory and antioxidant activities. Sodium aescinate inhibits hepatocellular carcinoma growth by targeting CARMA3/NF-κB pathway.
S3771 Stachydrine Stachydrine (Proline betaine, L-stachydrine, Methyl hygrate betaine) is a quaternary ammonium derivative of proline that occurs widely in Medicago species. It is an osmoprotective compound found in urine. Stachydrine is a major constituent of Chinese herb leonurus heterophyllus sweet used to promote blood circulation and dispel blood stasis. Stachydrine can inhibit the NF-κB signal pathway.
Pharm Biol, 2022, 60(1):700-707
J Cell Mol Med, 2019, 10.1111/jcmm.14551
S3773 Tyrosol Tyrosol (4-Hydroxyphenylethanol, 4-Hydroxyphenethyl alcohol, 2-(4-Hydroxyphenyl)ethanol) is an antioxidant that is naturally present in several foods such as wines and green tea and is present most abundantly in olives. Tyrosol is a derivative of phenethyl alcohol. Tyrosol attenuates pro-inflammatory cytokines from cultured astrocytes and NF-κB activation. Anti-oxidative and anti-inflammatory effects.
S8483 CBL0137 HCl CBL0137 (CBLC137, Curaxin 137) HCl激活p53并抑制NF-kB,在细胞实验中,IC50分别为0.37 μM 和 0.47 μM。它还能抑制组蛋白分子伴侣FACT,FACT促进染色质转录复合体的形成。
Cancer Lett, 2021, 520:201-212
Cancer Lett, 2021, 499:232-242
bioRxiv, 2021, 10.1101/2021.04.20.440573
S3355 3-Hydroxyanthranilic acid 3-Hydroxyanthranilic Acid (3-HAA, 3-HANA)是一种色氨酸代谢物具有免疫调节作用,可能是通过抑制 PI3K/Akt/mTORNF-κB 活性,减少促炎性介质的产生。
S9374 2',5'-Dihydroxyacetophenone 2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) 是二羟基苯乙酮异构体的混合物,用于食品调味。2',5'-Dihydroxyacetophenone 通过抑制 iNOS 的表达来显着抑制 NO 的产生。2',5'-Dihydroxyacetophenone 可通过阻断 ERK1/2NF-κB 信号通路来显著地降低促炎细胞因子 TNF-αIL-6 的表达水平。
Pathol Oncol Res, 2019, 25(1):301-309
S3871 Muscone Muscone (3-Methylcyclopentadecanone, Methylexaltone)是一种增香成分,一种有机化合物,是麝香气味的主要来源,也是一种有效的消炎剂。Muscone 可显著地下调LPDM诱导的炎症细胞因子水平,并抑制BMDM中 NF-κBNLRP3 炎性小体的活化。Muscone 还可以显著地降低炎性细胞因子inflammatory cytokines (IL-1β, TNF-α, IL-6) 的水平。
J Pharm Pharmacol, 2019, 71(11):1706-1713
S9388 (+)-Praeruptorin A Praeruptorin A is a coumarin compound naturally occurring in the roots of Peucedanum praeruptorum Dunn., a commonly used traditional Chinese medicine for the treatment of certain respiratory diseases and hypertension. Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κB activation. (+)-Praeruptorin A is one of enantiomers.
S9075 Mulberroside A Mulberroside A 是从 Morus alba 根的乙醇提取物中分离出的,具有抗酪氨酸酶和抗氧化活性,并被广泛用作化妆品中的活性成分。Mulberroside A 降低 TNF-αIL-1βIL-6 的表达并抑制 NALP3caspase-1NF-κB 的激活以及 ERKJNKp38 的磷酸化。
S2321 Magnolol Magnolol (NSC 293099) 是一种在Houpu magnolia (Magnolia officinalis) 树皮中发现的生物活性化合物。它能抑制TNFα诱导的NF-KB的激活。
Reprod Biol, 2021, 21(4):100567
Neoplasia, 2020, 22(11):576-589
J Chromatogr A, 2020, 1625:461230
S7637 DTP3 DTP3 是一种选择性GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7)抑制剂并能恢复 MKK7/JNK 的激活。DTP3 能够抑制癌症选择性NF-κB存活途径。
S3874 Curcumenol Curcumenol, a sesquiterpene isolated from Curcuma zedoaria, is known to possess a variety of health and medicinal values which includes neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. It inhibits NF-κB activation by suppressing the nuclear translocation of the NF-κB p65 subunit and blocking IκBα phosphorylation and degradation.
J Bone Miner Res, 2021, 10.1002/jbmr.4328
Int J Mol Med, 2021, 48(4)192
S1825 Erdosteine Erdosteine (KW-9144)是一种祛痰剂,用于治疗过多粘稠的粘液。Erdosteine 可抑制lipopolysaccharide (LPS)诱导的 NF-κB 激活。
S3880 Schisantherin A Schisantherin A (Gomisin C, Schisanwilsonin H, Arisanschinin K)是一种五味子红素,具有止咳、镇静、消炎、抗骨质疏松、神经保护、增强认知和心脏保护活性。Schisantherin A 也可通过IκBα降解抑制p65-NF-κB向核内移位。
S8341 TAK-243 (MLN7243) TAK-243 (MLN7243)是有效的ubiquitin activating enzyme (UAE)抑制剂,在UBCH10 E2硫代酸酯测定中IC50为1 ± 0.2 nM。在激酶和受体库中的选择性检验中,它对脱靶靶点包括I型和II型人源碳酸酐酶的抑制作用微弱。TAK-243 (MLN7243)可诱导ER stress,抑制NFκB信号通路的激活并促进凋亡。
Cell Rep, 2022, 38(12):110538
Free Radic Biol Med, 2022, 183:89-103
Arch Toxicol, 2022, 10.1007/s00204-021-03195-w
S6671 SN50 SN50 (NF-κB SN50)是一种可渗透细胞的NF-κB抑制肽,由Kaposi成纤维细胞生长因子信号肽组成。SN50抑制NF-κB的活化并减轻呼吸机诱发的肺损伤。
Cell Death Dis, 2021, 12(8):715
Int J Mol Sci, 2021, 22(16)8410
Behav Brain Res, 2021, 418:113647
S6679 C25-140 C25-140是TRAF6-Ubc13 interaction的小分子抑制剂。C25-140直接与TRAF6结合,从而阻止TRAF6与Ubc13的相互作用,因此降低了TRAF6的活性。C25-140还可在人和鼠原代细胞的各种免疫和炎性信号通路中阻碍NF-κB 激活。
S9417 Homoplantaginin Homoplantaginin (Hispidulin-7-glucoside) 是中草药丹参中的主要类黄酮,具有抗炎和抗氧化作用。Homoplantaginin 可抑制 TNF-αIL-6 mRNA 表达,IKKβNF-κB 磷酸化。
S4763 4-Hydroxychalcone 4-Hydroxychalcone (P-Cinnamoylphenol) is a chalcone metabolite with diverse biological activities. It inhibits TNFα-induced NF-κB pathway activation in a dose-dependent manner and also activates BMP signaling.
Oncol Lett, 2021, 21(3):213
S9871 BTYNB BTYNB (BTYNB IMP1 Inhibitor, MDK6620) 是一种有效且选择性的 IMP1c-Myc mRNA结合的抑制剂。BTYNB 可下调β-TrCP1 mRNA并降低 nuclear transcriptional factors-kappa B (NF-κB)的激活。BTYNB 通过损害IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA关联来破坏这种增强子功能。
S9106 Eleutheroside E Eleutheroside E, a principal component of Eleutherococcus senticosus (ES), has anti-inflammatory effects by inhibiting NF-κB and protecting against myocardial infarction.
S4460 IMM-H007 IMM-H007 是一种腺苷衍生物,是 AMP-Activated Protein Kinase (AMPK) 的激活剂。IMM-H007 是一种治疗心功能不全的潜在药物。IMM-H007 可通过钝化 NF-κBJNK/AP1 信号传导负向调节内皮炎症。IMM-H007 可抑制 ABCA1 (ATP binding cassette subfamily a member 1) 的降解并促进其在巨噬细胞中的细胞表面定位,从而促进胆固醇外流。
S3808 Mangiferin Mangiferin (Alpizarin, Chinomin, Hedysarid) is a bioactive compound that demonstrates many health perspectives and has been used to prepare medicinal and food supplements. Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50.
S5579 Chelidonic acid Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) 是在几种植物中发现的次级代谢产物,对实验动物的过敏性疾病具有治疗潜力。Chelidonic acid 通过阻断HMC-1细胞中的 NF-κBcaspase-1 来抑制 IL-6 的产生。Chelidonic acid 也是 glutamate decarboxylase 的抑制剂,其Ki值为1.2 μM。
S2341 (-)-Parthenolide (-)-Parthenolide, Nuclear Factor-κB抑制剂,可特异性地耗尽HDAC1蛋白,而不影响其他I/II类 HDACs。促进MDM2的泛素化并激活p53的细胞功能。
PLoS Genet, 2021, 17(11):e1009890
Theranostics, 2020, 10(22):9923-9936
J Biol Chem, 2020, 295(11):3576-3589
S3810 Scutellarin Scutellarin (Breviscapine, Breviscapin, Scutellarein-7-glucuronide)是从中草药黄芩Scutellaria baicalensis和灯盏细辛Erigeron breviscapus中提取的主要活性类黄酮,具有许多药理作用,例如抗氧化、抗肿瘤、抗病毒和抗炎活性。Scutellarin 可以下调HCC细胞中的 STAT3/Girdin/Akt 信号传导,并抑制破骨细胞中RANKL介导的 MAPKNF-κB 信号通路。
S8941 NIK SMI1 NIK SMI1 是一种高效的、选择性强的 NF-κB-inducing kinase (NIK) 的抑制剂,Ki值为0.23 nM,可用于NIK催化ATP水解为ADP。
S3604 Triptolide (PG490) Triptolide (PG490, NSC 163062)是一种三环氧二萜类化合物,是从中草药雷公藤中提取的免疫抑制剂。它是一种NF-κB抑制剂,抑制NF-κB转录活性,破坏p65/CBP的相互作用,减少p65蛋白。Triptolide (PG490) 可抑制 heat shock transcription factor 1 (HSF1) 的反式激活。Triptolide 可抑制 MDM2 并通过一个p53非依赖性通路来诱导凋亡。
Kidney Int, 2022, S0085-2538(22)00369-6
Ann N Y Acad Sci, 2022, 10.1111/nyas.14760
Sci Adv, 2021, 7(7)eabd2645
S3607 Sarsasapogenin Sarsasapogenin (SAR, Parigenin)是一种甾体皂甙元,能够诱发ROS的产生并激活unfolded protein response (UPR)信号通路。SAR能够有效地抑制NF-κBMAPK的激活,在LPS刺激的巨噬细胞中抑制IRAK1、TAK1和IκBα的磷酸化。
S3811 Ginsenoside Re Ginsenoside Re (Ginsenoside B2, Panaxoside Re, Sanchinoside Re, Chikusetsusaponin Ivc)是三七的提取物、人参中的主要人参皂苷,属于20(S)-原人参三醇组 (protopanaxatriol group)。它具有多种体外和体内作用,包括血管舒张作用,抗氧化剂,抗高血脂和血管生成作用。Ginsenoside Re 会降低 β-amyloid protein (Aβ) 并通过抑制 JNKNF-κB 起到抗炎的作用。
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3138 Methylthiouracil Methylthiouracil (NSC-193526, NSC-9378) 是一种抗甲状腺药。Methylthiouracil 可抑制 TNF-αIL-6 的产生以及 NF-κBERK1/2 的激活。
S3899 Hederagenin Hederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. Hederagenin inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB.
S9502 Madecassic acid Madecassic acid (Brahmic acid) 是最早从积雪草中分离的天然三萜,具有多种消炎和抗糖尿病作用,阻断巨噬细胞中的 NF-κB 活化并导致 iNOSCOX-2TNF-alphaIL-1betaIL-6 抑制。
S0454 Adjudin Adjudin (AF-2364) 是一种有效的男性避孕药,也是一种有效的 Cl⁻ channels 的阻滞剂。Adjudin 通过抑制 NF-κB p65核易位和DNA结合活性以及 ERK MAPK磷酸化而具有抗炎特性。
Brain Res Bull, 2022, 182:80-89
S9141 Berbamine Berbamine (BA, BBM) 是一种从中草药黄芦木中分离而来的双苄基异喹啉类天然产物。它是bcr/abl的新型抑制剂,具有有效的抗白血病活性,是NF-κB的抑制剂。Berbamine (BA, BBM) 通过靶向 Ca²⁺/calmodulin-dependent protein kinase II (CaMKII) 抑制癌细胞的生长,并诱导人骨髓瘤细胞凋亡。
Onco Targets Ther, 2019, 12:11437-11451
S1321 Urolithin B Urolithin B 通过减少 IκBα 的磷酸化和降解来抑制 NF-κB 活性。Urolithin B 可抑制 JNKERKAkt 的磷酸化,并增强 AMPK 的磷酸化。Urolithin B 也是 skeletal muscle mass 的调节剂。
S5453 Hyperoside Hyperoside (Hyperin, Quercetin 3-galactoside), a naturally occuring flavonoid compound, exerts multiple bioactivities, including myocardial protection, anti-redox, and anti-inflammatory activities.Hyperoside can inhibit activation of the NF-κB signaling pathway.
Ann Transl Med, 2021, 9(15):1233
Phytomedicine, 2021, 80:153387
J Agric Food Chem, 2021, 10.1021/acs.jafc.1c06292
S3867 (E)-Cardamonin (E)-Cardamonin (Alpinetin chalcone, cardamomin) is a naturally occurring chalcone with strong anti-inflammatory activity. It is a novel TRPA1 antagonist with IC50 of 454 nM and also a NF-kB inhibitor.
S6714 INH14 INH14是TLR2介导的NF-kB激活抑制剂,对IKKα和IKKβ的IC50值分别为8.975 μM和3.598 μM。
S3261 Myrislignan Myrislignan 是一种分离自Myristica fragrans Houtt的木脂素并具有抗炎活性。Myrislignan 可抑制 interleukin-6 (IL-6)tumour necrosis factor-α (TNF-α)。Myrislignan 剂量依赖性地抑制LPS刺激的巨噬细胞中 inducible NO synthase (iNOS)cyclooxygenase-2 (COX-2) 的表达。Myrislignan 可抑制 NF-κB 信号通路的激活。
S3872 Guaiacol Guaiacol (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.
S4712 Diethylmaleate Diethylmaleate (Diethyl ester, Maleic acid diethyl ester) 是Nrf2的激活剂,是马来酸的二乙酯形式,能消耗谷胱甘肽并抑制NFkB。
S3298 Caulophylline (N-Methylcytisine) Caulophylline (N-Methylcytisine, Caulophyllin, NMC) 是一种具有抗炎活性的三环喹喔啉生物碱。Caulophylline 可与鱿鱼视神经节的 nicotinic acetylcholine receptors (nAChR) 结合,Kd值为50 nM。Caulophylline 可显著地降低 myeloperoxidase (MPO) 的活性,并通过抑制 IκBIKK 磷酸化来阻断 NF-κB 的活化。
S9170 Engeletin Engeletin (Dihydrokaempferol 3-rhamnoside), a bioactive flavonoid, has multiple biological activities such as anti-diabetic and anti-inflammatory effects. engeletin againsts LPS-stimulated endometritis in mice via negative regulation of pro-inflammatory mediators via the TLR4-regulated NF-κB pathway.
Biochem Biophys Res Commun, 2020, 526(2):497-504
S3923 Ginsenoside Rg1 Ginsenoside Rg1 (Ginsenoside A2, Panaxoside A, Panaxoside Rg1, Sanchinoside C1, Sanchinoside Rg1)是人参的主要活性成分之一,被确定为原人参三醇型,对多种癌症具有药理作用,例如神经保护和抗肿瘤作用。Ginsenoside Rg1 可降低 cerebral Aβ 水平并减少 NF-κB 核转移。
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3924 Ginsenoside Rb1 Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.
J Biol Chem, 2021, S0021-9258(21)00790-0
Mol Immunol, 2021, 139:140-152
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3256 Tectochrysin Tectochrysin (Techtochrysin, NSC 80687) 是Alpinia oxyphylla Miquel的主要类黄酮之一。Tectochrysin 可显著地增加DR3DR4Fas的表达,并抑制 NF-κB 的活性。Tectochrysin 可诱导细胞凋亡。
S3609 Berbamine dihydrochloride Berbamine (BA, BBM) dihydrochloride 是一种从中草药黄芦木中分离而来的双苄基异喹啉类天然产物。它是bcr/abl的新型抑制剂,具有有效的抗白血病活性,是NF-κB的抑制剂。Berbamine (BA, BBM) dihydrochloride 通过靶向 Ca²⁺/calmodulin-dependent protein kinase II (CaMKII) 抑制癌细胞的生长,并诱导人骨髓瘤细胞凋亡。
S3299 Demethyleneberberine Demethyleneberberine (DMB) 是黄柏Cortex Phellodendri Chinensis (CPC) 的成分,可显著地缓解体重减轻并降低 myeloperoxidase (MPO) 活性,同时显著地减少促炎细胞因子的生成,例如 interleukin (IL)-6tumor necrosis factor-α (TNF-α),并抑制 NF-κB 信号通路的激活。Demethyleneberberine (DMB) 可以通过激活 AMPK 途径改善NAFLD (非酒精性脂肪肝疾病)。
S3603 Betulinic acid Betulinic acid (ALS-357, Lupatic acid, Betulic acid)是一种天然的五环三萜类化合物,具有抗病毒,抗疟药,抗发炎和抗肿瘤的特性。Betulinic acid也是 NF-kB 的活化剂。Phase 1/2
Mol Ther Nucleic Acids, 2022, 28:435-449
Oxid Med Cell Longev, 2021, 2021:5519587
J Cardiovasc Pharmacol, 2021, 78(2):235-246
S2979 CU-T12-9 CU-T12-9 是一种 Toll-like receptor (TLR) 1/2 的特异性激动剂,在 HEK-Blue hTLR2 SEAP 试验中EC50值为52.9 nM。CU-T12-9 可激活先天性和适应性免疫系统。CU-T12-9 可通过 NF-κB 发出信号并引起下游效应物 TNF-αIL-10iNOS 的升高。
E0211New Dihydroberberine Dihydroberberine是小檗碱 (BBR) 的氢化衍生物,通过双重调节 NF-κB 和 MAPK 信号通路发挥抗炎作用。
S4611 TCEP Hydrochloride TCEP (Tris(2-carboxyethyl)phosphine) hydrochloride 是一种非硫醇还原剂,可以以剂量相关的方式来促进NF-κB-DNA的结合。
S0949 Cucurbitacin IIb Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) 可抑制 STAT3JNKErk1/2 的磷酸化,而增强 IκBNF-κB 的磷酸化,阻止 NF-κB 的核易位并降低 IκBαTNF-α 的mRNA表达水平。Cucurbitacin IIb 是从Hemsleya amabilis 中分离出来的,具有抗炎活性并可诱导凋亡。
S5804 N-Acetylcysteine amide N-acetylcysteine amide是一种能穿透细胞膜的抗氧化剂,具有消炎活性,能够调节NF-κB的激活、HIF-1α和ROS。
Nat Commun, 2021, 12(1):647
Int J Biochem Cell Biol, 2020, 121:105703
Pancreatology, 2019, 19(2):258-265
S9184 Forsythoside B Forsythoside B 是从中药民间植物轮枝(Lamiophlomis rotata Kudo)的叶子中分离出来的一种苯乙胺类苷。Forsythoside B 具有有效的神经保护作用,并具有抗发炎、抗氧化和防腐特性。Forsythoside B 可以抑制 TNF-alphaIL-6IκB 并调节 NF-κB
S0844 NDMC101 NDMC101抑制破骨细胞的生成,从而改善爪肿胀和炎症性骨破坏,此过程与抑制NF-κB和NFATc1等转录因子以及多种蛋白激酶,包括p38、ERK和JNK有关。
S2371 Vanillylacetone Vanillylacetone (NSC 15335) 在化学结构上与其他香料,如Vanillin 和 Eugenol类似,用来作为一种香味味添加剂。Vanillylacetone (Zingerone) 可减轻氧化应激和炎症,下调NF-κB介导的信号通路。Zingerone 充当抗有丝分裂剂,并抑制神经母细胞瘤细胞的生长。
S1013 Bortezomib (PS-341) Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239)是有效的蛋白酶抑制剂,Ki为0.6 nM。它对肿瘤细胞表现出良好的选择性。Bortezomib (PS-341) 可抑制 NF-κB 并诱导 ERK 的磷酸化从而抑制cathepsin B并在卵巢癌和其他固体肿瘤中抑制自噬的催化过程。
Mol Cell, 2022, S1097-2765(22)00433-6
Sci Immunol, 2022, 7(68):eabi6763
Sci Adv, 2022, 8(4):eabi7711
S2824 TPCA-1 TPCA-1 (GW683965)是一种IKK-2抑制剂,无细胞试验中IC50为17.9 nM,抑制NF-κB通路,比作用于IKK-1选择性高22倍。TPCA-1 也是 STAT3 的抑制剂并可促进凋亡。
Nat Cell Biol, 2022, 24(5):766-782
Sci Adv, 2022, 8(12):eabh4050
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
S4902 QNZ (EVP4593) QNZ (EVP4593)有效抑制NF-κB激活和TNF-α产生,在Jurkat T细胞中IC50分别为11 nM和7 nM。
Cell Death Differ, 2022, 10.1038/s41418-022-00940-1
Cell Death Dis, 2022, 13(5):495
Cell Death Dis, 2022, 13(4):420
S8078 Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) 是一种IKK抑制剂,具有强的促凋亡和抗炎活性。同时还是有效的Nrf2激活剂和NF-κB抑制剂。Bardoxolone Methyl 可抑制铁死亡。Bardoxolone Methyl 在癌细胞中可诱导凋亡和自噬。
Drug Des Devel Ther, 2021, 15:21-35
Cancers (Basel), 2020, 12(6):E1645
Antioxidants (Basel), 2020, 9(1)
S1623 Acetylcysteine (N-acetylcysteine) Acetylcysteine (N-acetyl-l-cysteine, NAC)是ROS抑制剂,拮抗多种蛋白酶体抑制剂的活性。它还是肿瘤坏死因子TNF的抑制剂,主要用作祛痰剂,可通过维持或恢复肝脏中谷胱甘肽的浓度来处理扑热息痛(对乙酰氨基酚过量)。Acetylcysteine(N-acetyl-l-cysteine) 通过抑制IκB kinases抑制TNF诱导的NF-κB活化。Acetylcysteine(N-acetyl-l-cysteine) 通过线粒体依赖性途径诱导凋亡并抑制铁死亡和病毒复制。现配现用
EMBO Mol Med, 2022, 14(2):e14903
J Exp Clin Cancer Res, 2022, 41(1):41
Environ Sci Technol, 2022, 10.1021/acs.est.2c00585
E2661New Chitosan oligosaccharide Chitosan oligosaccharide (COS)是β-(1➔4)连接的d-氨基葡萄糖的低聚物,其作用涉及几个重要的途径的调节,包括抑制核因子κB (nuclear factor kappa B, NF-κB)丝裂原活化蛋白激酶(mitogen-activated protein kinases, MAPK),以及活化AMP -活化蛋白激酶(AMP-activated protein kinase, AMPK)
E0796New NF-κB-IN-1 NF-κB-IN-1是一种有效的NF-κB信号通路抑制剂,通过直接抑制抑制性κB激酶(inhibitory κB kinase, IKK)起作用。
E0783New SM-7368 SM-7368是一种有效的NF-κB抑制剂,可靶向MAPK p38激活的下游,也能抑制TNF-α诱导的MMP-9上调。
E0526New sappanone A Sappanone A是从豆科苏木心材中分离得到的一种异黄酮类化合物,通过p38 MAPK通路激活Nrf2,诱导HO-1表达,并通过抑制RelA/p65在Ser536位点的磷酸化来抑制脂多糖诱导的NF-κB的激活,发挥其抗炎作用。
S8989New Xanthatin Xanthatin是一种从中药苍耳(Xanthium strumarium)叶子中分离得到的倍半萜内酯,可抑制核因子kappa-B (nuclear factor kappa-B, NF-κB)、丝裂原活化蛋白激酶(mitogen-activated protein kinase, MAPK)以及信号转导和转录激活因子(signal transducer and activator of transcription, STATs)信号通路
E0212New Cornuside Cornuside 是一种从 Cornus officinalis SIEB. et ZUCC 果实中分离出来的双环烯醚萜苷化合物。Cornuside 通过抑制 RAW 264.7 巨噬细胞中的 NF-κB 活化来抑制脂多糖诱导的炎症介质。Cornuside 减弱大鼠皮质神经元的细胞凋亡。
E0022New Ophiopogonin D Ophiopogonin D (OJV-VI, Deacetylophiopogonin C) 是一种从中草药麦冬中分离得到的甾体糖苷,具有抗肿瘤作用。Ophiopogonin D 可通过调节 ITGB1/FAK/Src/AKT/β-catenin/MMP-9 信号轴抑制TGF-β1介导的MDA-MB-231细胞转移行为。Ophiopogonin D 还通过抑制小鼠肺上皮细胞中的 AMPK/NF-κB 通路来减轻 PM2.5 诱导的炎症。
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow)是流行的印度香料姜黄的主要姜黄色素,属于姜科(Zingiberaceae)。它是p300 histone acetylatransferase(IC50~25 μM)和Histone deacetylase (HDAC)的抑制剂,能够激活Nrf2 pathway并抑制NF-κB的激活。Curcumin 可诱导线粒体自噬、细胞自噬、凋亡和细胞周期阻滞,并具有抗肿瘤的活性。Curcumin 可通过减少铁死亡介导的细胞死亡来减少横纹肌溶解相关的肾衰竭。Curcumin 对各种人类病原体(如流感病毒,丙型肝炎病毒,HIV等)具有抗感染特性。
Phytother Res, 2022, 36(3):1326-1337
Dis Markers, 2022, 2022:3129781
Adv Sci (Weinh), 2021, e2103360
S4073 Sodium 4-Aminosalicylate Sodium 4-Aminosalicylate是一种用于治疗肺结核的抗生素,通过NF-κB的抑制和自由基清除起作用。
In Vitro Cell Dev Biol Anim, 2019, 55(5):368-375
PLoS One, 2016, 11(3):e0149754
S7351 JSH-23 JSH-23是一种NF-κB转录活性抑制剂,在RAW 264.7细胞系中IC50为7.1 μM。
Nat Cell Biol, 2022, 24(5):766-782
Int J Biol Sci, 2022, 18(5):2132-2145
Int J Mol Sci, 2022, 23(6)3280
S1576 Sulfasalazine (NSC 667219) Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) 是一种磺胺剂,是Mesalazine的衍生物,主要用作抗炎剂。Sulfasalazine 是一种有效的、特异性的 nuclear factor kappa B (NF-κB)TGF-βCOX-2 的抑制剂。Sulfasalazine 可诱导铁死亡、凋亡和自噬。
Cell Mol Life Sci, 2022, 79(5):228
Front Bioeng Biotechnol, 2022, 10:855755
Cell Metab, 2021, S1550-4131(21)00233-3
S7414 Caffeic Acid Phenethyl Ester Caffeic acid phenethyl ester (CAPE, Phenylethyl Caffeate)是强效的特异性NF-κB活化抑制剂,也能够表现出抗氧化、免疫调节和抗炎活动。
Oncogene, 2022, 10.1038/s41388-022-02253-6
Cancers (Basel), 2022, 14(2)274
J Exp Clin Cancer Res, 2021, 40(1):87
S3137 Sodium salicylate Sodium salicylate用来作为镇痛药和退烧药,是一种非甾类消炎药 (NSAID), 在癌细胞中可以诱导细胞凋亡和坏死。在转染的T细胞中,Sodium salicylate可以抑制 NF-kappa B的激活, 也可以抑制依赖NF-kappa B 的转录,包括Ig kappa 增强子 以及 人类免疫缺陷病毒 (HIV) 长末端重复序列(LTR)。
Theranostics, 2020, 10(17):7747-7757
S3939 4'-Methoxyresveratrol 4-Methoxyresveratrol is a stibenoid found in the Chinese herb Gnetum cleistostachyum. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation.
S4798 Benfotiamine Benfotiamine (S-Benzoylthiamine O-monophosphate) is a synthetic S-acyl derivative of thiamine (vitamin B1) and has been investigated for the treatment and prevention of Diabetic Nephropathy and Diabetes Mellitus, Type 2. Benfotiamine suppresses oxidative stress-induced NF-κB activation and prevents the bacterial endotoxin-induced inflammation.
J Mol Model, 2022, 28(6):153
S0002 IAXO-102 IAXO-102 是一种靶向MD-2和CD14共同受体的 TLR4 的拮抗剂。IAXO-102 可抑制 MAPK 和p65 NF-κB 磷酸化,并下调TLR4依赖性促炎蛋白的表达。IAXO-102 可抑制实验性腹主动脉瘤 (AAA) 的发展。
S6899 Licochalcone D Licochalcone D (Lico D, LCD, LD) 是一种从中草药甘草 Glycyrrhiza inflata 中分离出的类黄酮,具有抗氧化、抗炎和抗癌的特性。Licochalcone D 可抑制LPS信号通路中NF-κB p65的磷酸化。Licochalcone D 可抑制 JAK2EGFRMet (c-Met) 活性,并诱导ROS依赖性的凋亡。Licochalcone D 还可诱导 caspases 的活化和 poly (ADP-ribose) polymerase (PARP) 的裂解。
S8279 Shikonin (C.I. 75535) Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844)是一种 Pyruvate kinase M2 (PKM2) 有效的、特异的抑制剂。它是紫草的主要成分,紫草是一种中草药,具有多种生物活性。在细胞荧光淬灭试验中,Shikonin也是TMEM16A氯离子通道的抑制剂。Shikonin 通过抑制 tumor necrosis factor-α (TNF-α) 发挥抗炎作用,并可通过抑制 proteasome 来阻止 nuclear factor-κB (NF-κB) 信号途径的激活。
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Mil Med Res, 2022, 9(1):22
S0911 Hypaphorine Hypaphorine 大量存在于王不留行vaccaria semen中,通过抑制 ERK 或/和NFκB信号通路来抵消炎症。
S7672 Omaveloxolone (RTA-408) Omaveloxolone (RTA-408)是一种合成的三萜类化合物,其激活细胞保护转录因子 Nrf2 并抑制 NF-κB 信号。Phase 2。
Brain Behav, 2021, 11(1):e01918
Cancers (Basel), 2020, 12(9)E2668
Int J Neurosci, 2020, 7:1-16
S3223 L-Quebrachitol L-Quebrachitol (L-QCT) 是可从许多植物中分离出来的天然产物,促进增殖和细胞DNA合成。L-Quebrachitol 可上调 bone morphogenetic protein-2 (BMP-2)runt-related transcription factor-2 (Runx2)mitogen-activated protein kinase (MAPK) 相关调控基因和 Wnt/β-catenin 信号通路,同时下调 nuclear factor-κB(NF-κB) 配体 (RANKL) 受体激活剂的mRNA水平。
S3998 (+)-α-Lipoic acid (+)-α-Lipoic acid ((R)-(+)-α-Lipoic acid, α-Lipoic acid, Alpha-Lipoic acid)是thioctic acid的生理形式之一,是一种强效的抗氧化剂,可减轻糖尿病神经性症状。它比其外消旋体具有更优越的抗氧化性。R(+)-α-lipoic acid 是线粒体酶复合物的必要辅助因子。R(+)-α-lipoic acid 抑制 NF-κB 依赖性HIV-1 LTR 活化。
S0507 CBL0137 CBL0137 (Curaxin-137)是一种 histone chaperone FACT (facilitates chromatin transcription) 的抑制剂,可同时抑制 NF-κB 并激活 p53,对应的EC50值分别为0.47 μM和0.37 μM。
Cancer Lett, 2021, 520:201-212
Cancer Lett, 2021, 499:232-242
PLoS One, 2021, 16(6):e0252504
S5144 Neferine Neferine ((R)-1,2-Dimethoxyaporphine) 是 Nelumbo nucifera 的天然成分,具有抗肿瘤功效。Neferine 可诱导肾癌细胞凋亡。Neferine 通过激活肌肉细胞中的 Akt/mTOR 通路和 Nrf2 来防止自噬。Neferine 可抑制 NF-κB 的激活。Neferine具有多种治疗作用,例如抗糖尿病,抗衰老,抗微生物,抗血栓形成,抗心律不齐,抗炎甚至抗HIV。
Bone Res, 2022, 10(1):27
Oncol Rep, 2020, 44(3):1116-1126
S9208 Ginsenoside Rb3 Ginsenoside Rb3 是从人参中提取的天然产物,在心血管疾病包括心肌的缺血/再灌注(I/R)损伤中起着重要作用。在人肾293T细胞中检测了Ginsenoside Rb3(0.1-10 μM)对肿瘤坏死因子TNF-α诱导的 nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) 荧光素酶报告基因的抑制作用,IC50值为8.2 μM。在用10 ng/mL TNF-α处理后的HepG2细胞中,Ginsenoside Rb3 还以剂量依赖性的方式抑制 cyclooxygenase-2 (COX-2)inducible nitric oxide synthase (iNOS) 信使mRNA的诱导诱导表达。
S0923 Isoliquiritin apioside Isoliquiritin apioside (ISLA, ILA) 是一种分离自 Glycyrrhizae radix rhizome (GR) 的成分,可显著地降低PMA诱导的 matrix metalloproteinase (MMP) 的活性增加并抑制了PMA-诱导 mitogen-activated protein kinase (MAPK)NF-κB 的活化。Isoliquiritin apioside 在恶性癌细胞和EC中具有抗转移和抗血管生成的能力,并且没有细胞毒性。
S8961 Alobresib (GS-5829) Alobresib (GS-5829) 是一种新型的 BET 抑制剂,是一种针对复发/耐药的USC过表达c-Myc的高效治疗剂。Alobresib (GS-5829) 可抑制CLL细胞增殖并通过解除如 BLKAKTERK1/2MYC等关键信号通路的管制来诱导白血病细胞凋亡apoptosis。Alobresib (GS-5829) 还可抑制 NF-κB 的信号传导。
S3633 Pyrrolidinedithiocarbamate ammonium Pyrrolidinedithiocarbamate ammonium (Ammonium pyrrolidine dithiocarbamate, APDC, PDTC, Pyrrolidine dithiocarbamic acid ammonium salt)是NF-κB的有效抑制剂,抑制IκB磷酸化、阻止NF-κB易位入核并减少下游细胞因子的表达。
Signal Transduct Target Ther, 2022, 7(1):46
Cell Mol Life Sci, 2022, 79(2):86
Theranostics, 2022, 12(2):910-928
S0931 Jaceosidin Jaceosidin 是一种从Artemisia vestita中分离出来的类黄酮,在许多癌细胞中均具有抗肿瘤和抗增殖的活性。Jaceosidin 诱导凋亡,激活 Bax 并下调 Mcl-1c-FLIP 表达。Jaceosidin 可抑制 COX-2 的表达和 NF-κB 的激活。
S3901 Astragaloside IV Astragaloside IV (AST-IV, AS-IV) is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. AS-IV suppresses activation of p-Akt, p-mTOR, p-NF-κB and p-Erk1/2.
Naunyn Schmiedebergs Arch Pharmacol, 2020, 10.1007/s00210-020-02022-w
S3231 UCB-9260 UCB-9260 是一种口服活性抑制剂,可通过稳定三聚体的不对称形式来抑制 TNF 信号传导。 UCB-9260 与TNF结合的Kd值为13 nM。UCB-9260 还抑制TNF刺激后NF-κB,对应的IC50值为202 nM。
S3816 Dehydroevodiamine Dehydroevodiamine (DHED), a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.
S9244 8-O-acetyl shanzhiside methyl ester 8-O-acetyl shanzhiside methyl ester (Barlerin, ND01), isolated from the leaves of Lamiophlomis rotata Kudo, promotes angiogenesis, which leads to the improvement of functional outcome after stroke.8-O-Acetyl shanzhiside methyl ester can inhibts NF-κB.
S3384 (E/Z)-IT-603 (E/Z)-IT-603 是 E-IT-603 和 Z-IT-603的混合物。IT-603 是一种NF-κB 家族成员 c-Rel 抑制剂,在电泳迁移率变化试验 (EMSA) 中的 IC50 为 3 μM。
S5640 Ethyl caffeate Ethyl caffeate, a naturally occurring compound found in Bidens pilosa, suppresses NF-kappaB activation and its downstream inflammatory mediators, iNOS, COX-2 and PGE2 in vitro.
S0781 IQ 3 IQ 3 是一种特定的 c-Jun N-terminal kinase (JNK) 的抑制剂,对JNK3、JNK1和JNK2的Kd值分别为66 nM、240 nM和290 nM。IQ 3 可抑制TPS1-Blue细胞中LPS诱导的 NF-κB/AP1 的转录活性,IC50值为1.4 μM。IQ 3 还可以在体外实验中抑制 TNF-αIL-6 的产生。
S2261 Andrographolide Andrographolide是一种Labdane类二萜,是药用植物Andrographis paniculata的主要生物活性成分
Oxid Med Cell Longev, 2021, 2021:5577634
Int J Oncol, 2020, 56(6):1417-1428
Eur J Pharmacol, 2020, 873:172981
S2382 Evodiamine Evodiamine (Isoevodiamine)是Evodiae Fructus中提取的一种生物碱。它能通过抑制IkB kinase活性抑制NF-kB的激活。
Chem Biol Interact, 2021, 351:109756
Anticancer Drugs, 2021, 32(3):314-322
J Exp Clin Cancer Res, 2020, 39(1):249
S5771 Sulforaphane Sulforaphane 是一种天然存在的异硫氰酸盐,存在于十字花科蔬菜如西兰花、卷心菜、羽衣甘蓝。它是 Nrf2 的诱导物。Sulforaphane 也是 histone deacetylase (HDAC)NF-κB 的抑制剂。Sulforaphane 可增加 heme oxygenase-1 (HO-1),并降低 reactive oxygen species (ROS) 的水平。Sulforaphane 诱导细胞周期停滞和凋亡。
Elife, 2022, 11e67368
Cell Death Discov, 2021, 7(1):375
Cell Commun Signal, 2021, 19(1):35
S4937 4'-Hydroxychalcone 4'-Hydroxychalcone (P-Cinnamoylphenol),存在于草药、香料和茶叶中,是一种刺甘草查尔酮。它具有多种生物活性,能够抑制TNF-α诱导的NF-κB通路激活、并激活BMP信号通路。
S9295 Dauricine Dauricine, a plant metabolite isolated from the Asian vine Menispermum dauricum, plays a variety of biological roles in the human body, from inhibiting cancer cell growth to blocking cardiac transmembrane Na+, K+, and Ca2+ ion currents.Dauricine induces apoptosis, inhibits proliferation and invasion through inhibiting NF‐κB signaling pathway in colon cancer cells.
S5343 Vanillic acid Vanillic acid (4-hydroxy-3-methoxybenzoic acid) is a flavoring agent which is also an intermediate in the production of vanillin from ferulic acid. Vanillic acid inhibits NF-κB activation. Anti-inflammatory, antibacterial, and chemopreventive effects.
S2290 Dihydroartemisinin (DHA) Dihydroartemisinin (DHA, Dihydroqinghaosu, β-Dihydroartemisinin, Artenimol)是一种Artemisinin 的半合成衍生物,从传统中药Artemisia annua分离而来的。Dihydroartemisinin 可通过抑制 NF-κB 激活来诱导自噬和凋亡。
Front Pharmacol, 2022, 13:884881
Front Endocrinol (Lausanne), 2022, 13:891922
Nat Immunol, 2021, 10.1038/s41590-021-00967-5
S9193 Aristolochic acid A Aristolochic acid A (Aristolochic Acid I, Aristolochin, Aristolochine, TR 1736)是一种致癌、致突变和具有肾毒性的试剂,来源于马兜铃科的开花植物。Aristolochic acid A 可显著降低 activator protein 1 (AP-1)nuclear factor-κB (NF-κB) 的活性。
Mol Ther Nucleic Acids, 2020, 6;19:1276-1289
Am J Physiol Renal Physiol, 2020, 319(6):F1003-F1014
S7428 Rocaglamide Rocaglamide (Roc-A) 是从Aglaia物种中分离出来的一种有效的 heat shock factor 1 (HSF1) 活化的抑制剂,对HSF1的IC50值约为50 nM。Rocaglamide 可抑制翻译起始因子 eIF4A 的功能。Rocaglamide 还抑制 NF-κB 的活性。Rocaglamide 具有抗肿瘤活性。
S7445 E3330 E3330 (APX-3330)是一种有效的选择性APE1(Ref-1)抑制剂,其抑制 NF-κB DNA-结合活性。
Cell Death Dis, 2022, 13(2):124
Cancer Research on Prevention and Treatment, 2020, (7): 492-497
S2313 Indole-3-carbinol Indole-3-carbinol是通过降解硫代葡萄糖酸盐芸苔葡萄糖硫苷而来的,广泛存在于十字花科蔬菜中。它能够抑制NF-κBIκBα激酶的激活。
Am J Cancer Res, 2021, 11(10):4994-5005
J Med Virol, 2019, 91(8):1440-1447
S3931 Ginsenoside Rd Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S9040 Maslinic acid Maslinic Acid (Crategolic Acid, 2α-Hydroxyoleanoic Acid), a Natural Triterpene, exerts a wide range of biological activities, i.e. antitumor, antidiabetic, antioxidant, cardioprotective, neuroprotective, antiparasitic and growth-stimulating. MA significantly suppresses the DNA-binding activity of NF-κB p65 in LPS-induced RAW 264.7 cells.
S8587 Withaferin A Withaferin A (WA, WFA)可通过对硫代烷基化敏感的氧化还原机制阻止肿瘤坏死因子诱导的IκB激酶β的激活,从而有效地抑制 NF-κB 激活。Withaferin A 可与中间丝状体蛋白(IF) vimentin 结合,并具有抗肿瘤和抗血管生成活性。Withaferin A 是一种从 Withania somnifera 分离的甾体内酯。
Antioxidants (Basel), 2021, 10(7)1063
Mol Cell Biol, 2021, MCB0046721
bioRxiv, 2021, 10.1101/2021.02.04.429815
S7273 SC75741 SC75741 是强效的NF-κB抑制剂,其EC50为200 nM。SC75741 可有效地阻断流感病毒的传播。
Front Immunol, 2022, 13:839460
Int J Mol Sci, 2022, 23(6)3280
Microbiol Spectr, 2022, e0188121
S3760 Stachydrine hydrochloride Stachydrine is isolated from seed husk and the pulp of the fruit of C. Leonurus, and many other Asian plants and fruits. It has potent anti-metastatic activity and cardioprotective effects. Stachydrine hydrochloride is the major active constituent of Herba Leonuri, which is a potential therapy for cardiovascular diseases. Stachydrine can inhibit the NF-κB signal pathway. Anti-hypertrophic activities.
Pharm Biol, 2022, 60(1):700-707
S5899 (R)-(-)-Ibuprofen (R)-(-)-Ibuprofen ((R)-Ibuprofen) 可抑制T细胞刺激下 NF-κB 的激活,其IC50值为121.8 μM,且具有抗炎和镇痛作用。
S3293 Gardenoside Gardenoside 是一种从Gardenia栀子属果实中提取的天然化合物,具有保肝作用。Gardenoside 可抑制 TNF-αIL-1βIL-6NFκB 的活化。Gardenoside 还对游离脂肪酸(FFA)诱导的细胞脂肪变性具有抑制作用。Gardenoside 可通过调节 P2X3P2X7 受体来减轻慢性压迫性损伤大鼠的疼痛。
S3770 Sodium Aescinate Sodium Aescinate (SA, Escin Sodium Salt) is a widely-applied triterpene saponin product derived from horse chestnut seeds, possessing vasoactive and organ-protective activities with oral or injection administration in the clinic. Sodium aescinate is a triterpene saponin derived from Aesculus hippocastanum seeds, with anti-inflammatory and antioxidant activities. Sodium aescinate inhibits hepatocellular carcinoma growth by targeting CARMA3/NF-κB pathway.
S3771 Stachydrine Stachydrine (Proline betaine, L-stachydrine, Methyl hygrate betaine) is a quaternary ammonium derivative of proline that occurs widely in Medicago species. It is an osmoprotective compound found in urine. Stachydrine is a major constituent of Chinese herb leonurus heterophyllus sweet used to promote blood circulation and dispel blood stasis. Stachydrine can inhibit the NF-κB signal pathway.
Pharm Biol, 2022, 60(1):700-707
J Cell Mol Med, 2019, 10.1111/jcmm.14551
S3773 Tyrosol Tyrosol (4-Hydroxyphenylethanol, 4-Hydroxyphenethyl alcohol, 2-(4-Hydroxyphenyl)ethanol) is an antioxidant that is naturally present in several foods such as wines and green tea and is present most abundantly in olives. Tyrosol is a derivative of phenethyl alcohol. Tyrosol attenuates pro-inflammatory cytokines from cultured astrocytes and NF-κB activation. Anti-oxidative and anti-inflammatory effects.
S8483 CBL0137 HCl CBL0137 (CBLC137, Curaxin 137) HCl激活p53并抑制NF-kB,在细胞实验中,IC50分别为0.37 μM 和 0.47 μM。它还能抑制组蛋白分子伴侣FACT,FACT促进染色质转录复合体的形成。
Cancer Lett, 2021, 520:201-212
Cancer Lett, 2021, 499:232-242
bioRxiv, 2021, 10.1101/2021.04.20.440573
S3355 3-Hydroxyanthranilic acid 3-Hydroxyanthranilic Acid (3-HAA, 3-HANA)是一种色氨酸代谢物具有免疫调节作用,可能是通过抑制 PI3K/Akt/mTORNF-κB 活性,减少促炎性介质的产生。
S9374 2',5'-Dihydroxyacetophenone 2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) 是二羟基苯乙酮异构体的混合物,用于食品调味。2',5'-Dihydroxyacetophenone 通过抑制 iNOS 的表达来显着抑制 NO 的产生。2',5'-Dihydroxyacetophenone 可通过阻断 ERK1/2NF-κB 信号通路来显著地降低促炎细胞因子 TNF-αIL-6 的表达水平。
Pathol Oncol Res, 2019, 25(1):301-309
S3871 Muscone Muscone (3-Methylcyclopentadecanone, Methylexaltone)是一种增香成分,一种有机化合物,是麝香气味的主要来源,也是一种有效的消炎剂。Muscone 可显著地下调LPDM诱导的炎症细胞因子水平,并抑制BMDM中 NF-κBNLRP3 炎性小体的活化。Muscone 还可以显著地降低炎性细胞因子inflammatory cytokines (IL-1β, TNF-α, IL-6) 的水平。
J Pharm Pharmacol, 2019, 71(11):1706-1713
S9388 (+)-Praeruptorin A Praeruptorin A is a coumarin compound naturally occurring in the roots of Peucedanum praeruptorum Dunn., a commonly used traditional Chinese medicine for the treatment of certain respiratory diseases and hypertension. Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κB activation. (+)-Praeruptorin A is one of enantiomers.
S9075 Mulberroside A Mulberroside A 是从 Morus alba 根的乙醇提取物中分离出的,具有抗酪氨酸酶和抗氧化活性,并被广泛用作化妆品中的活性成分。Mulberroside A 降低 TNF-αIL-1βIL-6 的表达并抑制 NALP3caspase-1NF-κB 的激活以及 ERKJNKp38 的磷酸化。
S2321 Magnolol Magnolol (NSC 293099) 是一种在Houpu magnolia (Magnolia officinalis) 树皮中发现的生物活性化合物。它能抑制TNFα诱导的NF-KB的激活。
Reprod Biol, 2021, 21(4):100567
Neoplasia, 2020, 22(11):576-589
J Chromatogr A, 2020, 1625:461230
S7637 DTP3 DTP3 是一种选择性GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7)抑制剂并能恢复 MKK7/JNK 的激活。DTP3 能够抑制癌症选择性NF-κB存活途径。
S3874 Curcumenol Curcumenol, a sesquiterpene isolated from Curcuma zedoaria, is known to possess a variety of health and medicinal values which includes neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. It inhibits NF-κB activation by suppressing the nuclear translocation of the NF-κB p65 subunit and blocking IκBα phosphorylation and degradation.
J Bone Miner Res, 2021, 10.1002/jbmr.4328
Int J Mol Med, 2021, 48(4)192
S1825 Erdosteine Erdosteine (KW-9144)是一种祛痰剂,用于治疗过多粘稠的粘液。Erdosteine 可抑制lipopolysaccharide (LPS)诱导的 NF-κB 激活。
S3880 Schisantherin A Schisantherin A (Gomisin C, Schisanwilsonin H, Arisanschinin K)是一种五味子红素,具有止咳、镇静、消炎、抗骨质疏松、神经保护、增强认知和心脏保护活性。Schisantherin A 也可通过IκBα降解抑制p65-NF-κB向核内移位。
S8341 TAK-243 (MLN7243) TAK-243 (MLN7243)是有效的ubiquitin activating enzyme (UAE)抑制剂,在UBCH10 E2硫代酸酯测定中IC50为1 ± 0.2 nM。在激酶和受体库中的选择性检验中,它对脱靶靶点包括I型和II型人源碳酸酐酶的抑制作用微弱。TAK-243 (MLN7243)可诱导ER stress,抑制NFκB信号通路的激活并促进凋亡。
Cell Rep, 2022, 38(12):110538
Free Radic Biol Med, 2022, 183:89-103
Arch Toxicol, 2022, 10.1007/s00204-021-03195-w
S6671 SN50 SN50 (NF-κB SN50)是一种可渗透细胞的NF-κB抑制肽,由Kaposi成纤维细胞生长因子信号肽组成。SN50抑制NF-κB的活化并减轻呼吸机诱发的肺损伤。
Cell Death Dis, 2021, 12(8):715
Int J Mol Sci, 2021, 22(16)8410
Behav Brain Res, 2021, 418:113647
S6679 C25-140 C25-140是TRAF6-Ubc13 interaction的小分子抑制剂。C25-140直接与TRAF6结合,从而阻止TRAF6与Ubc13的相互作用,因此降低了TRAF6的活性。C25-140还可在人和鼠原代细胞的各种免疫和炎性信号通路中阻碍NF-κB 激活。
S9417 Homoplantaginin Homoplantaginin (Hispidulin-7-glucoside) 是中草药丹参中的主要类黄酮,具有抗炎和抗氧化作用。Homoplantaginin 可抑制 TNF-αIL-6 mRNA 表达,IKKβNF-κB 磷酸化。
S4763 4-Hydroxychalcone 4-Hydroxychalcone (P-Cinnamoylphenol) is a chalcone metabolite with diverse biological activities. It inhibits TNFα-induced NF-κB pathway activation in a dose-dependent manner and also activates BMP signaling.
Oncol Lett, 2021, 21(3):213
S9871 BTYNB BTYNB (BTYNB IMP1 Inhibitor, MDK6620) 是一种有效且选择性的 IMP1c-Myc mRNA结合的抑制剂。BTYNB 可下调β-TrCP1 mRNA并降低 nuclear transcriptional factors-kappa B (NF-κB)的激活。BTYNB 通过损害IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA关联来破坏这种增强子功能。
S9106 Eleutheroside E Eleutheroside E, a principal component of Eleutherococcus senticosus (ES), has anti-inflammatory effects by inhibiting NF-κB and protecting against myocardial infarction.
S4460 IMM-H007 IMM-H007 是一种腺苷衍生物,是 AMP-Activated Protein Kinase (AMPK) 的激活剂。IMM-H007 是一种治疗心功能不全的潜在药物。IMM-H007 可通过钝化 NF-κBJNK/AP1 信号传导负向调节内皮炎症。IMM-H007 可抑制 ABCA1 (ATP binding cassette subfamily a member 1) 的降解并促进其在巨噬细胞中的细胞表面定位,从而促进胆固醇外流。
S3808 Mangiferin Mangiferin (Alpizarin, Chinomin, Hedysarid) is a bioactive compound that demonstrates many health perspectives and has been used to prepare medicinal and food supplements. Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50.
S5579 Chelidonic acid Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) 是在几种植物中发现的次级代谢产物,对实验动物的过敏性疾病具有治疗潜力。Chelidonic acid 通过阻断HMC-1细胞中的 NF-κBcaspase-1 来抑制 IL-6 的产生。Chelidonic acid 也是 glutamate decarboxylase 的抑制剂,其Ki值为1.2 μM。
S2341 (-)-Parthenolide (-)-Parthenolide, Nuclear Factor-κB抑制剂,可特异性地耗尽HDAC1蛋白,而不影响其他I/II类 HDACs。促进MDM2的泛素化并激活p53的细胞功能。
PLoS Genet, 2021, 17(11):e1009890
Theranostics, 2020, 10(22):9923-9936
J Biol Chem, 2020, 295(11):3576-3589
S3810 Scutellarin Scutellarin (Breviscapine, Breviscapin, Scutellarein-7-glucuronide)是从中草药黄芩Scutellaria baicalensis和灯盏细辛Erigeron breviscapus中提取的主要活性类黄酮,具有许多药理作用,例如抗氧化、抗肿瘤、抗病毒和抗炎活性。Scutellarin 可以下调HCC细胞中的 STAT3/Girdin/Akt 信号传导,并抑制破骨细胞中RANKL介导的 MAPKNF-κB 信号通路。
S8941 NIK SMI1 NIK SMI1 是一种高效的、选择性强的 NF-κB-inducing kinase (NIK) 的抑制剂,Ki值为0.23 nM,可用于NIK催化ATP水解为ADP。
S3604 Triptolide (PG490) Triptolide (PG490, NSC 163062)是一种三环氧二萜类化合物,是从中草药雷公藤中提取的免疫抑制剂。它是一种NF-κB抑制剂,抑制NF-κB转录活性,破坏p65/CBP的相互作用,减少p65蛋白。Triptolide (PG490) 可抑制 heat shock transcription factor 1 (HSF1) 的反式激活。Triptolide 可抑制 MDM2 并通过一个p53非依赖性通路来诱导凋亡。
Kidney Int, 2022, S0085-2538(22)00369-6
Ann N Y Acad Sci, 2022, 10.1111/nyas.14760
Sci Adv, 2021, 7(7)eabd2645
S3607 Sarsasapogenin Sarsasapogenin (SAR, Parigenin)是一种甾体皂甙元,能够诱发ROS的产生并激活unfolded protein response (UPR)信号通路。SAR能够有效地抑制NF-κBMAPK的激活,在LPS刺激的巨噬细胞中抑制IRAK1、TAK1和IκBα的磷酸化。
S3811 Ginsenoside Re Ginsenoside Re (Ginsenoside B2, Panaxoside Re, Sanchinoside Re, Chikusetsusaponin Ivc)是三七的提取物、人参中的主要人参皂苷,属于20(S)-原人参三醇组 (protopanaxatriol group)。它具有多种体外和体内作用,包括血管舒张作用,抗氧化剂,抗高血脂和血管生成作用。Ginsenoside Re 会降低 β-amyloid protein (Aβ) 并通过抑制 JNKNF-κB 起到抗炎的作用。
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3138 Methylthiouracil Methylthiouracil (NSC-193526, NSC-9378) 是一种抗甲状腺药。Methylthiouracil 可抑制 TNF-αIL-6 的产生以及 NF-κBERK1/2 的激活。
S3899 Hederagenin Hederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. Hederagenin inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB.
S9502 Madecassic acid Madecassic acid (Brahmic acid) 是最早从积雪草中分离的天然三萜,具有多种消炎和抗糖尿病作用,阻断巨噬细胞中的 NF-κB 活化并导致 iNOSCOX-2TNF-alphaIL-1betaIL-6 抑制。
S0454 Adjudin Adjudin (AF-2364) 是一种有效的男性避孕药,也是一种有效的 Cl⁻ channels 的阻滞剂。Adjudin 通过抑制 NF-κB p65核易位和DNA结合活性以及 ERK MAPK磷酸化而具有抗炎特性。
Brain Res Bull, 2022, 182:80-89
S9141 Berbamine Berbamine (BA, BBM) 是一种从中草药黄芦木中分离而来的双苄基异喹啉类天然产物。它是bcr/abl的新型抑制剂,具有有效的抗白血病活性,是NF-κB的抑制剂。Berbamine (BA, BBM) 通过靶向 Ca²⁺/calmodulin-dependent protein kinase II (CaMKII) 抑制癌细胞的生长,并诱导人骨髓瘤细胞凋亡。
Onco Targets Ther, 2019, 12:11437-11451
S1321 Urolithin B Urolithin B 通过减少 IκBα 的磷酸化和降解来抑制 NF-κB 活性。Urolithin B 可抑制 JNKERKAkt 的磷酸化,并增强 AMPK 的磷酸化。Urolithin B 也是 skeletal muscle mass 的调节剂。
S5453 Hyperoside Hyperoside (Hyperin, Quercetin 3-galactoside), a naturally occuring flavonoid compound, exerts multiple bioactivities, including myocardial protection, anti-redox, and anti-inflammatory activities.Hyperoside can inhibit activation of the NF-κB signaling pathway.
Ann Transl Med, 2021, 9(15):1233
Phytomedicine, 2021, 80:153387
J Agric Food Chem, 2021, 10.1021/acs.jafc.1c06292
S3867 (E)-Cardamonin (E)-Cardamonin (Alpinetin chalcone, cardamomin) is a naturally occurring chalcone with strong anti-inflammatory activity. It is a novel TRPA1 antagonist with IC50 of 454 nM and also a NF-kB inhibitor.
S6714 INH14 INH14是TLR2介导的NF-kB激活抑制剂,对IKKα和IKKβ的IC50值分别为8.975 μM和3.598 μM。
S3261 Myrislignan Myrislignan 是一种分离自Myristica fragrans Houtt的木脂素并具有抗炎活性。Myrislignan 可抑制 interleukin-6 (IL-6)tumour necrosis factor-α (TNF-α)。Myrislignan 剂量依赖性地抑制LPS刺激的巨噬细胞中 inducible NO synthase (iNOS)cyclooxygenase-2 (COX-2) 的表达。Myrislignan 可抑制 NF-κB 信号通路的激活。
S3872 Guaiacol Guaiacol (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.
S4712 Diethylmaleate Diethylmaleate (Diethyl ester, Maleic acid diethyl ester) 是Nrf2的激活剂,是马来酸的二乙酯形式,能消耗谷胱甘肽并抑制NFkB。
S3298 Caulophylline (N-Methylcytisine) Caulophylline (N-Methylcytisine, Caulophyllin, NMC) 是一种具有抗炎活性的三环喹喔啉生物碱。Caulophylline 可与鱿鱼视神经节的 nicotinic acetylcholine receptors (nAChR) 结合,Kd值为50 nM。Caulophylline 可显著地降低 myeloperoxidase (MPO) 的活性,并通过抑制 IκBIKK 磷酸化来阻断 NF-κB 的活化。
S9170 Engeletin Engeletin (Dihydrokaempferol 3-rhamnoside), a bioactive flavonoid, has multiple biological activities such as anti-diabetic and anti-inflammatory effects. engeletin againsts LPS-stimulated endometritis in mice via negative regulation of pro-inflammatory mediators via the TLR4-regulated NF-κB pathway.
Biochem Biophys Res Commun, 2020, 526(2):497-504
S3923 Ginsenoside Rg1 Ginsenoside Rg1 (Ginsenoside A2, Panaxoside A, Panaxoside Rg1, Sanchinoside C1, Sanchinoside Rg1)是人参的主要活性成分之一,被确定为原人参三醇型,对多种癌症具有药理作用,例如神经保护和抗肿瘤作用。Ginsenoside Rg1 可降低 cerebral Aβ 水平并减少 NF-κB 核转移。
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3924 Ginsenoside Rb1 Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.
J Biol Chem, 2021, S0021-9258(21)00790-0
Mol Immunol, 2021, 139:140-152
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3256 Tectochrysin Tectochrysin (Techtochrysin, NSC 80687) 是Alpinia oxyphylla Miquel的主要类黄酮之一。Tectochrysin 可显著地增加DR3DR4Fas的表达,并抑制 NF-κB 的活性。Tectochrysin 可诱导细胞凋亡。
S3609 Berbamine dihydrochloride Berbamine (BA, BBM) dihydrochloride 是一种从中草药黄芦木中分离而来的双苄基异喹啉类天然产物。它是bcr/abl的新型抑制剂,具有有效的抗白血病活性,是NF-κB的抑制剂。Berbamine (BA, BBM) dihydrochloride 通过靶向 Ca²⁺/calmodulin-dependent protein kinase II (CaMKII) 抑制癌细胞的生长,并诱导人骨髓瘤细胞凋亡。
S3299 Demethyleneberberine Demethyleneberberine (DMB) 是黄柏Cortex Phellodendri Chinensis (CPC) 的成分,可显著地缓解体重减轻并降低 myeloperoxidase (MPO) 活性,同时显著地减少促炎细胞因子的生成,例如 interleukin (IL)-6tumor necrosis factor-α (TNF-α),并抑制 NF-κB 信号通路的激活。Demethyleneberberine (DMB) 可以通过激活 AMPK 途径改善NAFLD (非酒精性脂肪肝疾病)。
S3603 Betulinic acid Betulinic acid (ALS-357, Lupatic acid, Betulic acid)是一种天然的五环三萜类化合物,具有抗病毒,抗疟药,抗发炎和抗肿瘤的特性。Betulinic acid也是 NF-kB 的活化剂。Phase 1/2
Mol Ther Nucleic Acids, 2022, 28:435-449
Oxid Med Cell Longev, 2021, 2021:5519587
J Cardiovasc Pharmacol, 2021, 78(2):235-246
S2979 CU-T12-9 CU-T12-9 是一种 Toll-like receptor (TLR) 1/2 的特异性激动剂,在 HEK-Blue hTLR2 SEAP 试验中EC50值为52.9 nM。CU-T12-9 可激活先天性和适应性免疫系统。CU-T12-9 可通过 NF-κB 发出信号并引起下游效应物 TNF-αIL-10iNOS 的升高。
E0211New Dihydroberberine Dihydroberberine是小檗碱 (BBR) 的氢化衍生物,通过双重调节 NF-κB 和 MAPK 信号通路发挥抗炎作用。
S4611 TCEP Hydrochloride TCEP (Tris(2-carboxyethyl)phosphine) hydrochloride 是一种非硫醇还原剂,可以以剂量相关的方式来促进NF-κB-DNA的结合。
S0949 Cucurbitacin IIb Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) 可抑制 STAT3JNKErk1/2 的磷酸化,而增强 IκBNF-κB 的磷酸化,阻止 NF-κB 的核易位并降低 IκBαTNF-α 的mRNA表达水平。Cucurbitacin IIb 是从Hemsleya amabilis 中分离出来的,具有抗炎活性并可诱导凋亡。
S5804 N-Acetylcysteine amide N-acetylcysteine amide是一种能穿透细胞膜的抗氧化剂,具有消炎活性,能够调节NF-κB的激活、HIF-1α和ROS。
Nat Commun, 2021, 12(1):647
Int J Biochem Cell Biol, 2020, 121:105703
Pancreatology, 2019, 19(2):258-265
S9184 Forsythoside B Forsythoside B 是从中药民间植物轮枝(Lamiophlomis rotata Kudo)的叶子中分离出来的一种苯乙胺类苷。Forsythoside B 具有有效的神经保护作用,并具有抗发炎、抗氧化和防腐特性。Forsythoside B 可以抑制 TNF-alphaIL-6IκB 并调节 NF-κB
E2661New Chitosan oligosaccharide Chitosan oligosaccharide (COS)是β-(1➔4)连接的d-氨基葡萄糖的低聚物,其作用涉及几个重要的途径的调节,包括抑制核因子κB (nuclear factor kappa B, NF-κB)丝裂原活化蛋白激酶(mitogen-activated protein kinases, MAPK),以及活化AMP -活化蛋白激酶(AMP-activated protein kinase, AMPK)
E0796New NF-κB-IN-1 NF-κB-IN-1是一种有效的NF-κB信号通路抑制剂,通过直接抑制抑制性κB激酶(inhibitory κB kinase, IKK)起作用。
E0783New SM-7368 SM-7368是一种有效的NF-κB抑制剂,可靶向MAPK p38激活的下游,也能抑制TNF-α诱导的MMP-9上调。
E0526New sappanone A Sappanone A是从豆科苏木心材中分离得到的一种异黄酮类化合物,通过p38 MAPK通路激活Nrf2,诱导HO-1表达,并通过抑制RelA/p65在Ser536位点的磷酸化来抑制脂多糖诱导的NF-κB的激活,发挥其抗炎作用。
S8989New Xanthatin Xanthatin是一种从中药苍耳(Xanthium strumarium)叶子中分离得到的倍半萜内酯,可抑制核因子kappa-B (nuclear factor kappa-B, NF-κB)、丝裂原活化蛋白激酶(mitogen-activated protein kinase, MAPK)以及信号转导和转录激活因子(signal transducer and activator of transcription, STATs)信号通路
E0212New Cornuside Cornuside 是一种从 Cornus officinalis SIEB. et ZUCC 果实中分离出来的双环烯醚萜苷化合物。Cornuside 通过抑制 RAW 264.7 巨噬细胞中的 NF-κB 活化来抑制脂多糖诱导的炎症介质。Cornuside 减弱大鼠皮质神经元的细胞凋亡。
E0022New Ophiopogonin D Ophiopogonin D (OJV-VI, Deacetylophiopogonin C) 是一种从中草药麦冬中分离得到的甾体糖苷,具有抗肿瘤作用。Ophiopogonin D 可通过调节 ITGB1/FAK/Src/AKT/β-catenin/MMP-9 信号轴抑制TGF-β1介导的MDA-MB-231细胞转移行为。Ophiopogonin D 还通过抑制小鼠肺上皮细胞中的 AMPK/NF-κB 通路来减轻 PM2.5 诱导的炎症。
E0211New Dihydroberberine Dihydroberberine是小檗碱 (BBR) 的氢化衍生物,通过双重调节 NF-κB 和 MAPK 信号通路发挥抗炎作用。
Tags: NF-κB inhibitor|NF-κB agonist|NF-κB activator|NF-κB inducer|NF-κB antagonist|NF-κB signaling pathway|NF-κB assay kit