IκB/IKK
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
IκB/IKK产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1274 |
BX-795BX-795 是一种有效的，特异性的PDK1抑制剂，在无细胞试验中IC50为6 nM，作用于PDK1比作用于PKA和PKC选择性分别高140和1600倍。同时，相比于 GSK3β，作用于PDK1的选择性高出100多倍。BX-795 可通过抑制 ULK1 来调节自噬。BX-795 还是一种有效的 TBK1 抑制剂，可阻断 TBK1 和 IKKε，IC 50 值分别为 6 nM 和 41 nM。 |
Induction of basal p62 Ser403 phosphorylation in ULK1/2-deficient MEF was suppressed by BX-795, an inhibitor of TBK1. WT ( Ulk1 +/+/Ulk2 +/+) and Ulk1 -/- /Ulk2 -/-(KO) MEF were treated with NaCl/Pi (Con) or 10 uM BX-795 for 6 h, and subjected to immunoblotting with indicated antibodies.
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| S1396 |
Resveratrol (SRT501)Resveratrol (SRT501, trans-Resveratrol)具有广泛靶点，包括环氧酶（如COX, IC50=1.1 μM）、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素，具有抗癌，抗炎，降血糖和其他有益心血管的作用。Resveratrol可诱导线粒体自噬、细胞自噬和自噬依赖性的凋亡。 |
Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours. |
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| S2913 |
BAY 11-7082BAY 11-7082 (BAY 11-7821)是一种 NF-κB 抑制剂，抑制TNFα诱导的 IκBα 磷酸化，在肿瘤细胞中IC50为10 μM。BAY 11-7082 可抑制 ubiquitin-specific protease USP7 和 USP21，对应的IC50值分别为0.19 μM和0.96 μM。BAY 11-7082 在胃癌细胞中可诱导凋亡和S期阻滞。 |
Immunofluorescence images of Ishikawa cells showing the increase in the nuclear colocalization of ERa (red) and p65 (green) after E2 incubation. Nuclear colocalization is yellow. Treatment with ICI 182,780, PDTC or Bay inhibited the nuclear localization of both ERa and p65. Blue, DAPI-stained nuclei. All pictures were obtained the same day using the same microscope settings. Original magnification 3200, bar =50 um. Arrows, cytoplasmic ERa and p65 staining. ICI, ICI 182,780; Bay, Bay 11-7082.
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| S2882 |
IKK-16 (IKK Inhibitor VII)IKK-16 (IKK Inhibitor VII)是一种选择性的IκB激酶(IKK)抑制剂，作用于IKK-2，IKK complex和IKK-1，无细胞试验中IC50分别为40 nM，70 nM和200 nM。IKK-16 还可抑制细胞内LRRK2 Ser935的磷酸化和体外实验中LRRK2的激酶活性，对应的IC50值为50 nM。 |
Reduction in IFN-g production in TcREG by IKK-16 coincides with decrease in T-bet and Eomes expression levels. Flow cytometry plots showing cellular analysis for T-bet and Eomes in CD45+CD3+CD8+ population.
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| S2824 |
TPCA-1TPCA-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。 |
AGS cells were treated with cwith IL-1β in the presence of the IKK inhibitor TPCA-1, the p38 MAPK inhibitor BIX02188 and the JNK inhibitor SP600125. Cell lysates were obtained 24 h after IL-1β treatment and immunoblotted with PTEN antibodies. |
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| S6386New |
MRT67307MRT67307（IKKε/TBK1 Inhibitor II）抑制IKKϵ/TBK1，在体外ATP（终浓度 0.1 mM）实验中，其IC50分别为160和19 nM，但当其浓度为10 μM时，对 IKKα 和 IKKβ 没有抑制作用。MRT67307 也是 ULK1 和 ULK2的抑制剂 ，其IC50分别为45和38 nM。MRT67307可阻断细胞中的自噬（autophagy）。 |
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| S2864 |
IMD 0354IMD-0354 (IKK2 Inhibitor V)是一种IKKβ抑制剂，作用于NF-κβ通路，抑制IκBα磷酸化。 |
(B) Histological examinations of xenograft lesions produced by A549 cells. We stained the lesions with H&E, TUNEL and staining for Ki-67. (C, D) The histogram shows percentage of A549 cells that were positive for proliferation marker Ki-67 and apoptosis marker TUNEL in 3 representative fields. Results are expressed as the mean ± SD. ns. P > 0.05, **P < 0.01 and ***P < 0.001 for the indicated comparisons by 1-way A OVA or Student’s t test.
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| S8078 |
Bardoxolone MethylBardoxolone 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。 |
Renal Nrf2 activity was shown in RTA402-treated acFSGS (RTA402 + acFSGS) mice as early as day 7 (RTA402 + acFSGS) and persisted to day 28, compared to vehicle + acFSGS mice. Kidney in situ ROS production demonstrated by DHE detection.
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| S8044 |
BMS-345541BMS-345541是一种催化亚基的高选择性抑制剂，作用于IKK-2和IKK-1，无细胞试验中IC50分别为0.3 μM和4 μM。 |
(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. *, p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. *, p<0.05.
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| S4907 |
SC-514SC-514 (GK 01140)是一种口服有效的，ATP竞争性的IKK-2抑制剂，IC50为3-12 μM，抑制NF-κB依赖性的基因表达，不抑制其他IKK异构体或其他丝-苏氨酸和酪氨酸激酶。 |
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| S1681 |
Mesalamine (5-ASA)Mesalamine (5-Aminosalicylic acid, 5-ASA, Mesalazine, Apriso, Asacol, Pentasa, Canasa)是一种抗炎化合物。 |
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| S7352 |
Bay 11-7085BAY 11-7085 (Bay 11-7083) 是TNFα诱导的IκBα磷酸化的不可逆抑制剂，其IC50为10 μM。 |
VSMCs were pretreated with BAY 11-7085 (BAY, 10μmol/L) for 1h and further treated with or without 10-7mol/L salusin-β for 30min. A, Cytoplasmic extracts (Cy) were obtained and the phosphorylated IκBα, IκBα and HDCA3 protein levels were measured by western blot analysis. B, nuclear extracts (Nu) were obtained and the nuclear p50, p65 and HDAC3 protein levels were measured by western blot analysis. Data are expressed as means ± SD (n=3). *P< 0.05 versus the control with no treatment; #P< 0.05 versus 10-7mol/L salusin-β treatment alone.
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| S3615 |
Dehydrocostus LactoneDehydrocostus lactone (DHE)是一种天然的倍半萜内酯，抑制IKKβ活性、IκBα的磷酸化和降解、共激活子p300的招募、p50/p65 NF-κB的核转位及它们结合于COX2启动子上的能力。DHE具有抗炎、抗溃疡、抗肿瘤作用和免疫调节活性。 |
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| S0949 |
Cucurbitacin IIbCucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) 可抑制 STAT3、JNK 和 Erk1/2 的磷酸化，而增强 IκB 和 NF-κB 的磷酸化，阻止 NF-κB 的核易位并降低 IκBα 和 TNF-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。 |
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| S7851 |
AZD3264AZD3264是一种新型IKK2抑制剂。 |
(C) G361 cells were loaded with DCF (ROS probe) and further stimulated with vehicle or indicated IKKβ inhibitors for 3 h. Fluorescence was measured using a fluorescence microplate reader. *, p<0.05 versus control.
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| S3168 |
cis-Resveratrolcis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) 是Resveratrol的顺式异构体。Resveratrol 是一种天然的酚类化合物，具有抗氧化、抗炎、保护心脏和抗癌的特性。Resveratrol 是 pregnane X receptor (PXR) 的抑制剂，也是 Nrf2 和 SIRT1 的激活剂，并可能诱导凋亡。Resveratrol 还可抑制多种靶标，包括 5-lipoxygenase (LOX)、cyclooxygenase (COX)、IKKβ、DNA polymerases α和δ，IC50分别为2.7 μM、<1 μM、1 μM、3.3 μM和5 μM。 |
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| S7697 |
LY2409881LY2409881 是一种有效的选择性 IKK2 抑制剂，IC50 为 30 nM，选择性比IKK1和其他常见激酶高10倍多。 |
A549 cells were treated with NF-kB inhibitor LY2409881 (30 nM) for 2 h, followed by western blot analysis of p-NF-kB.
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| S7691 |
PS-1145PS-1145是一种特异性IKK抑制剂，IC50 为 88 nM。 |
(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. *, p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. *, p<0.05.
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| S3648 |
Amlexanox (AA-673)Amlexanox (AA-673, CHX-3673, Amoxanox)是一种抗炎抗过敏免疫调节剂，也是蛋白激酶 TBK1 和 IKK-ε 的抑制剂。 |
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| S7948 |
MRT67307 HClMRT67307是一种高效的双重的IKKϵ /TBK1抑制剂，其IC50分别为160和19 nM。MRT67307 可有效地抑制 ULK1 和 ULK2 并限制自噬。 |
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| S7736 |
MLN120BLN120B (ML120B) 是一种有效、选择性、可逆和 ATP 竞争性的 IkappaB 激酶β (IKKβ) 抑制剂，对重组 IKKβ 的 IC50 为 45 nM。MLN120B 在 IC50 低于 50 μM 时不抑制其他 IKK 同种型。 |
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| S9042 |
WedelolactoneWedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα. Wedelolactone is also an inhibitor of caspase-11. |
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| S9417 |
HomoplantagininHomoplantaginin (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-α 和 IL-6 mRNA 表达，IKKβ 和 NF-κB 磷酸化。 |
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| S0425 |
TBK1/IKKε-IN-2TBK1/IKKε-IN-2 (Ikk epsilon-in-1, IKKε-IN-1, MDK10496)是一种 TBK1 和 IKKε 的双重抑制剂。 |
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| S8935 |
BAY-985BAY-985是一种有效、高选择性的TBK1/IKKε抑制剂。 BAY-985对TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay)和IKKε (IC50 = 2 nM)具有高效力，在机械性细胞phosphorylation of interferon regulatory factor 3(pIRF3)分析中也具有高效力(IC50 = 74 nM)，并且对SK-MEL-2细胞具有抗增殖作用(IC50 = 900 nM)。 |
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| S3607 |
SarsasapogeninSarsasapogenin (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-κB和MAPK的激活，在LPS刺激的巨噬细胞中抑制IRAK1、TAK1和IκBα的磷酸化。 |
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| S8922 |
TBK1/IKKε-IN-1(compound 1)TBK1/IKKε-IN-5 (compound 1) 是一种 TANK-binding kinase 1 (TBK1) 和 IκB kinase-ε (IKKε/IKK-i) 的双重抑制剂，对于TBK1和IKKε的IC50值分别为1.0 nM和5.6 nM。TBK1 /IKKε被抑制可增强对PD-1阻断的反应，从而有效地预测了体内的肿瘤反应。 |
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| S1321 |
Urolithin BUrolithin 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 JNK、ERK 和 Akt 的磷酸化，并增强 AMPK 的磷酸化。Urolithin B 也是 skeletal muscle mass 的调节剂。 |
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| S6714 |
INH14INH14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。 |
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| 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 IκB 和 IKK 磷酸化来阻断 NF-κB 的活化。 |
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| S9184 |
Forsythoside BForsythoside 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-alpha、IL-6、IκB 并调节 NF-κB。 |
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| S3612 |
Rosmarinic acidRosmarinic acid (RA, Rosemary acid) 是一种天然的羟化化合物。它具有阻止补体结合、抑制脂肪氧合酶和环氧煤活性的功能，通过抑制NF-κB激活信号中IKK-β的活性、抑制CCL11和CCR3的表达。 |
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| S7441 |
WS3WS3是一种β细胞增殖诱导剂，通过调节Erb3 binding protein-1 (EBP1)和IκB kinase通路发挥作用。 |
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| S7442 |
WS6WS6通过调节Erb3 binding protein-1 (EBP1)和IκB kinase通路诱导β细胞增殖。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1274 |
BX-795BX-795 是一种有效的，特异性的PDK1抑制剂，在无细胞试验中IC50为6 nM，作用于PDK1比作用于PKA和PKC选择性分别高140和1600倍。同时，相比于 GSK3β，作用于PDK1的选择性高出100多倍。BX-795 可通过抑制 ULK1 来调节自噬。BX-795 还是一种有效的 TBK1 抑制剂，可阻断 TBK1 和 IKKε，IC 50 值分别为 6 nM 和 41 nM。 |
Induction of basal p62 Ser403 phosphorylation in ULK1/2-deficient MEF was suppressed by BX-795, an inhibitor of TBK1. WT ( Ulk1 +/+/Ulk2 +/+) and Ulk1 -/- /Ulk2 -/-(KO) MEF were treated with NaCl/Pi (Con) or 10 uM BX-795 for 6 h, and subjected to immunoblotting with indicated antibodies.
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| S1396 |
Resveratrol (SRT501)Resveratrol (SRT501, trans-Resveratrol)具有广泛靶点，包括环氧酶（如COX, IC50=1.1 μM）、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素，具有抗癌，抗炎，降血糖和其他有益心血管的作用。Resveratrol可诱导线粒体自噬、细胞自噬和自噬依赖性的凋亡。 |
Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours. |
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| S2913 |
BAY 11-7082BAY 11-7082 (BAY 11-7821)是一种 NF-κB 抑制剂，抑制TNFα诱导的 IκBα 磷酸化，在肿瘤细胞中IC50为10 μM。BAY 11-7082 可抑制 ubiquitin-specific protease USP7 和 USP21，对应的IC50值分别为0.19 μM和0.96 μM。BAY 11-7082 在胃癌细胞中可诱导凋亡和S期阻滞。 |
Immunofluorescence images of Ishikawa cells showing the increase in the nuclear colocalization of ERa (red) and p65 (green) after E2 incubation. Nuclear colocalization is yellow. Treatment with ICI 182,780, PDTC or Bay inhibited the nuclear localization of both ERa and p65. Blue, DAPI-stained nuclei. All pictures were obtained the same day using the same microscope settings. Original magnification 3200, bar =50 um. Arrows, cytoplasmic ERa and p65 staining. ICI, ICI 182,780; Bay, Bay 11-7082.
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| S2882 |
IKK-16 (IKK Inhibitor VII)IKK-16 (IKK Inhibitor VII)是一种选择性的IκB激酶(IKK)抑制剂，作用于IKK-2，IKK complex和IKK-1，无细胞试验中IC50分别为40 nM，70 nM和200 nM。IKK-16 还可抑制细胞内LRRK2 Ser935的磷酸化和体外实验中LRRK2的激酶活性，对应的IC50值为50 nM。 |
Reduction in IFN-g production in TcREG by IKK-16 coincides with decrease in T-bet and Eomes expression levels. Flow cytometry plots showing cellular analysis for T-bet and Eomes in CD45+CD3+CD8+ population.
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| S2824 |
TPCA-1TPCA-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。 |
AGS cells were treated with cwith IL-1β in the presence of the IKK inhibitor TPCA-1, the p38 MAPK inhibitor BIX02188 and the JNK inhibitor SP600125. Cell lysates were obtained 24 h after IL-1β treatment and immunoblotted with PTEN antibodies. |
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| S6386New |
MRT67307MRT67307（IKKε/TBK1 Inhibitor II）抑制IKKϵ/TBK1，在体外ATP（终浓度 0.1 mM）实验中，其IC50分别为160和19 nM，但当其浓度为10 μM时，对 IKKα 和 IKKβ 没有抑制作用。MRT67307 也是 ULK1 和 ULK2的抑制剂 ，其IC50分别为45和38 nM。MRT67307可阻断细胞中的自噬（autophagy）。 |
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| S2864 |
IMD 0354IMD-0354 (IKK2 Inhibitor V)是一种IKKβ抑制剂，作用于NF-κβ通路，抑制IκBα磷酸化。 |
(B) Histological examinations of xenograft lesions produced by A549 cells. We stained the lesions with H&E, TUNEL and staining for Ki-67. (C, D) The histogram shows percentage of A549 cells that were positive for proliferation marker Ki-67 and apoptosis marker TUNEL in 3 representative fields. Results are expressed as the mean ± SD. ns. P > 0.05, **P < 0.01 and ***P < 0.001 for the indicated comparisons by 1-way A OVA or Student’s t test.
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| S8078 |
Bardoxolone MethylBardoxolone 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。 |
Renal Nrf2 activity was shown in RTA402-treated acFSGS (RTA402 + acFSGS) mice as early as day 7 (RTA402 + acFSGS) and persisted to day 28, compared to vehicle + acFSGS mice. Kidney in situ ROS production demonstrated by DHE detection.
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| S8044 |
BMS-345541BMS-345541是一种催化亚基的高选择性抑制剂，作用于IKK-2和IKK-1，无细胞试验中IC50分别为0.3 μM和4 μM。 |
(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. *, p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. *, p<0.05.
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| S4907 |
SC-514SC-514 (GK 01140)是一种口服有效的，ATP竞争性的IKK-2抑制剂，IC50为3-12 μM，抑制NF-κB依赖性的基因表达，不抑制其他IKK异构体或其他丝-苏氨酸和酪氨酸激酶。 |
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| S1681 |
Mesalamine (5-ASA)Mesalamine (5-Aminosalicylic acid, 5-ASA, Mesalazine, Apriso, Asacol, Pentasa, Canasa)是一种抗炎化合物。 |
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| S7352 |
Bay 11-7085BAY 11-7085 (Bay 11-7083) 是TNFα诱导的IκBα磷酸化的不可逆抑制剂，其IC50为10 μM。 |
VSMCs were pretreated with BAY 11-7085 (BAY, 10μmol/L) for 1h and further treated with or without 10-7mol/L salusin-β for 30min. A, Cytoplasmic extracts (Cy) were obtained and the phosphorylated IκBα, IκBα and HDCA3 protein levels were measured by western blot analysis. B, nuclear extracts (Nu) were obtained and the nuclear p50, p65 and HDAC3 protein levels were measured by western blot analysis. Data are expressed as means ± SD (n=3). *P< 0.05 versus the control with no treatment; #P< 0.05 versus 10-7mol/L salusin-β treatment alone.
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| S3615 |
Dehydrocostus LactoneDehydrocostus lactone (DHE)是一种天然的倍半萜内酯，抑制IKKβ活性、IκBα的磷酸化和降解、共激活子p300的招募、p50/p65 NF-κB的核转位及它们结合于COX2启动子上的能力。DHE具有抗炎、抗溃疡、抗肿瘤作用和免疫调节活性。 |
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| S0949 |
Cucurbitacin IIbCucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) 可抑制 STAT3、JNK 和 Erk1/2 的磷酸化，而增强 IκB 和 NF-κB 的磷酸化，阻止 NF-κB 的核易位并降低 IκBα 和 TNF-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。 |
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| S7851 |
AZD3264AZD3264是一种新型IKK2抑制剂。 |
(C) G361 cells were loaded with DCF (ROS probe) and further stimulated with vehicle or indicated IKKβ inhibitors for 3 h. Fluorescence was measured using a fluorescence microplate reader. *, p<0.05 versus control.
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| S3168 |
cis-Resveratrolcis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) 是Resveratrol的顺式异构体。Resveratrol 是一种天然的酚类化合物，具有抗氧化、抗炎、保护心脏和抗癌的特性。Resveratrol 是 pregnane X receptor (PXR) 的抑制剂，也是 Nrf2 和 SIRT1 的激活剂，并可能诱导凋亡。Resveratrol 还可抑制多种靶标，包括 5-lipoxygenase (LOX)、cyclooxygenase (COX)、IKKβ、DNA polymerases α和δ，IC50分别为2.7 μM、<1 μM、1 μM、3.3 μM和5 μM。 |
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| S7697 |
LY2409881LY2409881 是一种有效的选择性 IKK2 抑制剂，IC50 为 30 nM，选择性比IKK1和其他常见激酶高10倍多。 |
A549 cells were treated with NF-kB inhibitor LY2409881 (30 nM) for 2 h, followed by western blot analysis of p-NF-kB.
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| S7691 |
PS-1145PS-1145是一种特异性IKK抑制剂，IC50 为 88 nM。 |
(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. *, p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. *, p<0.05.
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| S3648 |
Amlexanox (AA-673)Amlexanox (AA-673, CHX-3673, Amoxanox)是一种抗炎抗过敏免疫调节剂，也是蛋白激酶 TBK1 和 IKK-ε 的抑制剂。 |
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| S7948 |
MRT67307 HClMRT67307是一种高效的双重的IKKϵ /TBK1抑制剂，其IC50分别为160和19 nM。MRT67307 可有效地抑制 ULK1 和 ULK2 并限制自噬。 |
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| S7736 |
MLN120BLN120B (ML120B) 是一种有效、选择性、可逆和 ATP 竞争性的 IkappaB 激酶β (IKKβ) 抑制剂，对重组 IKKβ 的 IC50 为 45 nM。MLN120B 在 IC50 低于 50 μM 时不抑制其他 IKK 同种型。 |
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| S9042 |
WedelolactoneWedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα. Wedelolactone is also an inhibitor of caspase-11. |
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| S9417 |
HomoplantagininHomoplantaginin (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-α 和 IL-6 mRNA 表达，IKKβ 和 NF-κB 磷酸化。 |
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| S0425 |
TBK1/IKKε-IN-2TBK1/IKKε-IN-2 (Ikk epsilon-in-1, IKKε-IN-1, MDK10496)是一种 TBK1 和 IKKε 的双重抑制剂。 |
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| S8935 |
BAY-985BAY-985是一种有效、高选择性的TBK1/IKKε抑制剂。 BAY-985对TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay)和IKKε (IC50 = 2 nM)具有高效力，在机械性细胞phosphorylation of interferon regulatory factor 3(pIRF3)分析中也具有高效力(IC50 = 74 nM)，并且对SK-MEL-2细胞具有抗增殖作用(IC50 = 900 nM)。 |
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| S3607 |
SarsasapogeninSarsasapogenin (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-κB和MAPK的激活，在LPS刺激的巨噬细胞中抑制IRAK1、TAK1和IκBα的磷酸化。 |
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| S8922 |
TBK1/IKKε-IN-1(compound 1)TBK1/IKKε-IN-5 (compound 1) 是一种 TANK-binding kinase 1 (TBK1) 和 IκB kinase-ε (IKKε/IKK-i) 的双重抑制剂，对于TBK1和IKKε的IC50值分别为1.0 nM和5.6 nM。TBK1 /IKKε被抑制可增强对PD-1阻断的反应，从而有效地预测了体内的肿瘤反应。 |
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| S1321 |
Urolithin BUrolithin 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 JNK、ERK 和 Akt 的磷酸化，并增强 AMPK 的磷酸化。Urolithin B 也是 skeletal muscle mass 的调节剂。 |
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| S6714 |
INH14INH14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。 |
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| 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 IκB 和 IKK 磷酸化来阻断 NF-κB 的活化。 |
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| S9184 |
Forsythoside BForsythoside 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-alpha、IL-6、IκB 并调节 NF-κB。 |
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| S3612 |
Rosmarinic acidRosmarinic acid (RA, Rosemary acid) 是一种天然的羟化化合物。它具有阻止补体结合、抑制脂肪氧合酶和环氧煤活性的功能，通过抑制NF-κB激活信号中IKK-β的活性、抑制CCL11和CCR3的表达。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7441 |
WS3WS3是一种β细胞增殖诱导剂，通过调节Erb3 binding protein-1 (EBP1)和IκB kinase通路发挥作用。 |
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| S7442 |
WS6WS6通过调节Erb3 binding protein-1 (EBP1)和IκB kinase通路诱导β细胞增殖。 |
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