Caspase
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
Caspase产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
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| S2228 |
Belnacasan (VX-765)Belnacasan (VX-765)是一种有效的选择性caspase-1抑制剂，无细胞试验中Ki为0.8 nM。Phase 2。 |
(D and E) Caspase-1 inhibitors (Ac-YVAD-CMK and VX765) were added during the induction of trastuzumab-dependent BT-474 (red) or rituximab-dependent Raji cell phagocytosis (green). MFI of PD-L1 (D) and IDO (E) in macrophages are as indicated.
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| S6846New |
Gly-Phe β-naphthylamideGly-Phe β-naphthylamide (Gly-Phe beta-naphthylamide)是在溶酶体内积累的组织蛋白酶 C 的底物。Gly-Phe-β-naphthylamide 可以抑制 caspase-8 的组织蛋白酶依赖性激活。 |
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| S9817New |
Ac-FLTD-CMKAc-FLTD-CMK 是一种特异性的 inflammatory caspases 的抑制剂。Ac-FLTD-CMK 在体外通过 caspases-1、-4、-5 和 -11 抑制 gasdermin D (GSDMD) 裂解。Ac-FLTD-CMK 对caspases-1、caspases-4 和 caspases-5 的IC50值分别为 46.7 nM、1.49 μM 和 329 nM。 |
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| S2417 |
20-Hydroxyecdysone20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone, Crustecdysone) 是一种自然发生的蜕皮激素，控制节肢动物的蜕皮和变态。20-Hydroxyecdysone (Ecdysterone, 20E) 可抑制 caspase 活性并通过20E核受体复合体 EcR-USP 来诱导自噬。 |
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| S7023 |
Z-VAD-FMKZ-VAD-FMK (Z-VAD(OMe)-FMK)是一种细胞渗透性的，不可逆泛caspase抑制剂，在THP.1 和 Jurkat T细胞中阻断细胞凋亡的所有特性。 |
(A and B) Western blot analysis examining the effect of zVAD-fmk on the icaritin-induced apoptosis. The caspase inhibitor zVAD-fmk could significantly decrease the icaritin-induced cleaved caspase-3 expression. β-Actin protein levels indicate that an equal amount of protein was loaded into each lane.n=3. Mean±SD. bP<0.05, compared to the control group. eP<0.05, compared to the icaritin-treated group. |
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| S7314 |
Z-IETD-FMKZ-IETD-FMK (Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK)是一种特异性Caspase-8抑制剂。 |
The caspase-8 inhibitors do not rescue NB4 cells from TPEN-triggered apoptosis. NB4 cells were pre-treated with 50 μM Z-ITED-FMK or 100 μM Ac-IETD-CHO for 1 h, and then treated with 5 μM TPEN for 24 h. (A) Cell morphology was observed and recorded using an optical microscope. The scale bar represents 20 μm. A partiallty enlarged view was shown in the lower left corner of every picture. (B) Apoptosis rate was measured with Annexin V/PI dual staining by flow cytometry.
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| S7313 |
Z-LEHD-FMK TFAZ-LEHD-FMK TFA (Caspase-9 Inhibitor) 是一种具有细胞透性、不可逆的Caspase-9抑制剂，有助于细胞生存。 |
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| S3267 |
Kaempferol-3-O-rutinosideKaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside) 是从 Carthamus tinctorius 中提取的黄酮，可改变受伤神经元的形状和结构，减少凋亡细胞，下调 p-JAK2、p-STAT3、caspase-3 和 Bax 的表达，并降低Bax免疫反应性，并增加 Bcl-2 蛋白表达和免疫反应性。 |
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| S7312 |
Z-DEVD-FMKZ-DEVD-FMK (Caspase-3 Inhibitor)是一种特异性，不可逆的Caspase-3抑制剂，也能有效抑制caspase-6， caspase-7， caspase-8和caspase-10。 |
(J,K)After pre-treated with Caspase-3 inhibitor Z-DEVD-FMK 50μM, the apoptotic rates of cells induced by E Platinum in BGC-823, MGC-803, and SGC-7901 cells were detected by Annexin V/PI double-staining assay. Ann.V-/PI- as healthy cells, Ann.+/PI- as early apoptotic cells, Ann.+/PI+ probably as late apoptotic cells. Data were shown as means SD for three independent experiments (*P<0.05 and **P<0.01 compared with control, ##P<0.01 compared to Z-DEVD-FMK+40 μM E Platinum group with treatment of 40 μM E Platinum). |
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| S7311 |
Q-VD-OphQ-VD-OPh (Quinoline-Val-Asp-Difluorophenoxymethylketone)是一种有效的pan-caspase抑制剂，作用于caspases 1， 3， 8和9，IC50范围在25到400 nM之间，有效抑制与细胞凋亡相关的末端caspase激活，底物裂解，及DNA梯状条带形成。Q-VD-OPh 可抑制HIV感染。 |
UA and Q-VD-Oph attenuated TNF-α-induced unclear translocation of NF-κB (C) and P-STAT3(S727) (D) in BEAS-2B cells.
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| S3275 |
Senkyunolide ISenkyunolide I (SEI, SENI) 是一种从 Ligusticum chuanxiong 中提取的口服活性化合物，具有止痛、抗偏头痛、神经保护、抗氧化和抗凋亡的活性。Senkyunolide I (SEI, SENI) 可上调 Erk1/2 的磷酸化，并诱导 Nrf2 的核易位，伴随着HO-1和NQO1的表达增强。Senkyunolide I (SEI, SENI) 可提高 Bcl-2/Bax 的比例，并抑制裂化的 caspase 3 和 caspase 9 的表达。 |
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| S8507 |
Z-YVAD-FMKZ-YVAD-FMK 是一种具有抗炎和抗肿瘤活性的细胞渗透性的、不可逆的 caspase-1 特异性抑制剂。 |
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| S8102 |
Z-VAD(OH)-FMK (Caspase Inhibitor VI)Z-VAD(OH)-FMK (Caspase Inhibitor VI) 是一类不可逆的泛caspase抑制剂。 |
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-FMK-S810201Z0220161121.gif)
Effect on the RAS of CFZ, z-VAD-fmk, or CFZ+z-VAD-fmk treatments administered 5 or 12 days after C26 inoculation and control groups. Serum levels of a renin and b ANGII. c The mRNA expression of ATF2. d Western blot analysis of ATF2 and pATF2. e pATF2-to-ATF2 ratio. Significant differences were detected between most of the groups, with the exceptionsof (A and B) CP and UT (D) and ZP and ZT (#); and (C and E) CP and UP (*), CT and UT (#), and HC, ZP, ZT and CC (&). ZP:z-VAD-fmk.
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| S7775 |
Emricasan (IDN-6556)Emricasan (IDN-6556, PF 03491390, PF-03491390)是有效的、不可逆的泛半胱天冬酶（pan-caspase）抑制剂。Emricasan 也是寨卡病毒感染的抑制剂。 |
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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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| S9075 |
Mulberroside AMulberroside 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-α、IL-1β 和 IL-6 的表达并抑制 NALP3、caspase-1 和 NF-κB 的激活以及 ERK、JNK 和 p38 的磷酸化。 |
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| S7901 |
Ac-DEVD-CHOAc-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO)是Group II caspases的有效抑制剂，对caspase-3和caspase-7的Ki值分别为0.2 nM和1.6 nM。对caspase-2制剂效果弱，Ki值为1.7 μM。 |
Microwave (MW) hyperthermia triggers cell death through caspase-3-mediated apoptosis. H460, PC-9 and H1975 cells were treated with or without Ac-DEVD-CHO for 3 h prior to MW hyperthermia (43°C for 90 min), then allowed to recover at 37°C until 24 h. (A) Cell viability was determined by CCK-8 assay. Data are expressed as the means ± SEM of 3 independent experiments. *P<0.05 vs. the control group, **P<0.01 vs. the control group.
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| S5579 |
Chelidonic acidChelidonic 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-κB 和 caspase-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。 |
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| S5584 |
CitronellolCitronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells. |
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| S1029 |
Lenalidomide (CC-5013)Lenalidomide (CC-5013)是一种TNF-α分泌抑制剂，在PBMCs中IC50为13 nM。Lenalidomide (CC-5013) 是 ubiquitin E3 ligase cereblon (CRBN) 的配体，它通过CRBN-CRL4泛素连接酶引起两个淋巴样转录因子IKZF1和IKZF3的选择性泛素化和降解。Lenalidomide 可促进 cleaved caspase-3 的表达、抑制 VEGF 的表达并诱导凋亡。 |
Effect of lenalidomide treatment (50 mg/kg/day, p.o. for 3 days) on expression of tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), Fas, Fas ligand (FasL), and cleaved caspase-3 in myocardium from lean and ob/ob mice. (a) Representative gel blots of TNF-α, IL-6, Fas, FasL, cleaved caspase-3 and α-Tubulin (as loading control) using specific antibodies. (b) TNF-α. |
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| S2768 |
Dinaciclib (SCH727965)Dinaciclib (SCH727965, PS-095760) 是一种新型有效的CDK抑制剂，作用于CDK2，CDK5，CDK1和CDK9，无细胞试验中IC50分别为1 nM，1 nM，3 nM和4 nM。它也会阻断胸甘(dThd) DNA整合。Dinaciclib 可通过激活caspases 8和caspases 9来诱导细胞凋亡。Phase 3。 |
CDK4/6 inhibition has potent cytostatic effect in HER2-positive models. The indicated cells were treated with PD-0332991 (1 uM) or Dinaciclib (1 uM) for 96 hours and plates were stained with crystal violet.
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| S2738 |
PAC-1PAC-1是一种有效的procaspase-3（酶原-3）激活剂，EC50为0.22 μM，是第一个已知的直接激活酶原e-3为caspase-3的小分子。 |
The effects of PAC-1 (activator of ROS) administration on the newborn pups' weight and the plasma IGF-1 and ROS levels in graviditas gp91phox-/- mice. The values are presented as the means ± SD derived from six animals. *P<0.05 in comparison to the non-treatment mice.
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| S2891 |
GW441756GW441756 是一种有效的，选择性的TrkA抑制剂，IC50为2 nM，对c-Raf1和CDK2几乎没有抑制活性。GW441756 可增加caspase-3并诱导凋亡。 |
Thermal latency and mechanical allodynia were normalized in the RTXw1 + 4MC group (n= 6). In these mice, thermal hypoalgesia reappeared within 2 days of GW441756 injection (D). GW441756 did not affect mechanical thresholds (E) in the RTXw1 + 4MC group. (F, G) The diagrams show behavioral responses of naïve mice to either gambogic amide (open square, n = 6) or GW441756 (open circle, n =6). Gambogic amide induced mild thermal hyperalgesia within 2 days of injection but GW441756 did not affect thermal latencies (F). Both gambogic amide and GW441756 did not affect mechanical responses. *P < 0.05, **P < 0.01, and ***P < 0.001: paired t-test comparing preinjection vs. postinjection effects. #P < 0.05, ##P < 0.01, and ###P < 0.001: between drugs and saline treatments.
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| S2927 |
Apoptosis Activator 2Apoptosis Activator 2强诱导caspase-3激活， PARP分裂， DNA断裂，导致细胞破坏(Apaf-1依赖性的)，IC50约为4 μM，抑制HMEC， PREC和MCF-10A细胞活性。 |
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| S7326 |
TasisulamTasisulam (LY573636)是一种抗肿瘤剂，是通过内源途径导致细胞凋亡的诱导物。 Phase 3 |
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| S6899 |
Licochalcone DLicochalcone 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 JAK2、EGFR 和 Met (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。 |
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| S0913 |
4',5,7-Trimethoxyflavone4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) 是一种从 Kaempferia parviflora (KP) 分离的类黄酮，可诱导凋亡。4',5,7-Trimethoxyflavone 可增加亚G1期、DNA片段化、膜联蛋白-V/PI染色和Bax/Bcl-xL比，激活 caspase-3 并降解 poly (ADP-ribose) polymerase (PARP) 蛋白。 |
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| S6501 |
NVP 231NVP 231是新型CerK抑制剂，在体外抑制重组CerK的催化活性，IC50为12 nM。 |
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| S3238 |
ResibufogeninResibufogenin (Bufogenin, Recibufogenin) 是huachansu华蟾素中具有抗癌作用的成分，通过上调 receptor-interacting protein kinase 3 (RIP3) 和磷酸化 mixed lineage kinase domain-like protein 的Ser358位点来触发坏死病。Resibufogenin 可通过诱导 reactive oxygen species (ROS) 积累发挥细胞毒性作用。Resibufogenin 可诱导凋亡和 caspase-3 和 caspase-8 活性。Resibufogenin 增加 Bax/Bcl-2 表达，并抑制 cyclin D1、cyclin E、PI3K、p-AKT、p-GSK3β 和 β-catenin 的蛋白表达。 |
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| S9276 |
Alisol BAlisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways. |
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| S2271 |
Berberine chloride (NSC 646666)Berberine chloride (NSC 646666, Natural Yellow 18)是异喹啉类生物碱的季铵盐。Berberine chloride 可激活 caspase 3 和 caspase 8，分裂 poly ADP-ribose polymerase (PARP) 和释放 cytochrome c。Berberine chloride 可降低 c-IAP1，Bcl-2 和 Bcl-XL 的表达。Berberine chloride 可通过 JNK 和 p38 MAPK 的持续磷酸化以及产生 ROS 来诱导凋亡。Berberine chloride 是一个 topoisomerase I 和 II 的双效抑制剂。Berberine chloride 也是一个潜在的自噬调节剂。 |
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| S2448 |
Gambogic AcidGambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin)激活caspases，EC50为0.78 - 1.64 μM，且完全抑制Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 和 Mcl-1，IC50分别为1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM 和 0.79 μM。 |
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| S5967 |
Berberine chloride hydrateBerberine (Natural Yellow 18) chloride hydrate 是属于异喹啉生物碱的季铵盐。Berberine 可激活 caspase 3 和 caspase 8，poly ADP-ribose polymerase (PARP) 的切割和 cytochrome c 的释放。Berberine chloride 可降低 c-IAP1、Bcl-2 和 Bcl-XL 的表达。Berberine chloride 通过 JNK 和 p38 MAPK 的持续磷酸化以及 ROS的生成来诱导凋亡。Berberine chloride 是一种 topoisomerase I 和 II 的双重抑制剂。Berberine chloride 也是一种潜在的自噬调节剂。 |
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| S0354 |
AlsterpaulloneAlsterpaullone (Alp, 9-Nitropaullone, NSC 705701) 是一种 CDK 的有效抑制剂，对CDK1/cyclin B、CDK2/cyclin A、CDK2/cyclin E 和 CDK5/p35的IC50值分别为35 nM、15 nM、200 nM和40 nM。Alsterpaullone 还可作为 glycogen synthase kinase-3 (GSK-3) 的有效抑制剂，对GSK-3α和GSK-3β的IC50值均为4 nM。Alsterpaullone 可通过激活 caspase-9 诱导凋亡。Alsterpaullone 具有抗肿瘤活性，具有治疗神经退行性和增生性疾病的潜力。 |
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| S4513 |
RGD peptide (GRGDNP)RGD peptide (GRGDNP) 是 integrins 与细胞外基质结合的抑制剂。RGD peptide (GRGDNP) 可能通过直接激活 caspase-3 并诱导凋亡。 |
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| S9097 |
Alisol B AcetateAlisol B acetate, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways. |
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| S5550 |
Ethyl gallateEthyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity. |
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| S6990 |
PhytohemagglutininPhytohemagglutinin (PHA, Phaseolus vulgaris agglutinin) 在毕赤酵母中利用天然信号肽或酿酒酵母α-因子前体序列表达，将蛋白质引导至分泌途径。Phytohemagglutinin 可通过增加凋亡蛋白 Bax 和激活 caspases-3 来诱导人HEp-2癌细胞的凋亡。 |
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| S9634 |
Phenoxodiol (Haginin E)Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) 是一种具有抗肿瘤活性的异黄酮类似物，可激活 caspase 系统，抑制 XIAP (X-linked inhibitor of apoptosis)，并破坏 FLICE inhibitory protein (FLIP) 的表达，从而导致肿瘤细胞凋亡。Phenoxodiol 也抑制 DNA topoisomerase II。 |
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| S4353 |
TerfenadineTerfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9. |
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| S3865 |
Taurochenodeoxycholic acidTaurochenodeoxycholic acid (Taurochenodeoxycholic acid (Taurochenodeoxycholate, TCDCA, Chenodeoxycholyltaurine)), a bile acid formed in the liver of most species, is used as a cholagogue and choleretic. |
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| S3224 |
CinobufaginCinobufagin (Cinobufagine) 是 Venenum Bufonis 的活性成分，可抑制肿瘤发展。Cinobufagin 可提高 ATM 和 Chk2 并降低 CDC25C、CDK1 和 cyclin B。Cinobufagin 抑制 PI3K、AKT 和 Bcl-2，同时增加裂解的 caspase-9 和 caspase-3 水平。由此诱导细胞周期停滞在G2/M期及凋亡。 |
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| S6882 |
HI-TOPK-032HI-TOPK-032 是一种有效的、特异性的 TOPK 的抑制剂。HI-TOPK-032 还可以降低 ERK-RSK 磷酸化，调节 p53、裂化的 caspase-7 和裂化的 PARP 的丰度，并在癌细胞中诱导凋亡。 |
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| S3088 |
(±)-Methyl Jasmonate(±)-Methyl Jasmonate (MeJA, Methyl jasmonate, Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate)，是一种植物激素，在植物中起着至关重要的细胞调节剂的作用，是调节炎症性肠病(IBDs)的新候选药物，可调节 caspase 型蛋白酶家族主要类型的表达。 |
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| S8487New |
AP20187AP20187 (B/B Homodimerizer, HY-13992) 是一种二聚化的化学诱导剂，可激活 FKBP-Casp8。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2228 |
Belnacasan (VX-765)Belnacasan (VX-765)是一种有效的选择性caspase-1抑制剂，无细胞试验中Ki为0.8 nM。Phase 2。 |
(D and E) Caspase-1 inhibitors (Ac-YVAD-CMK and VX765) were added during the induction of trastuzumab-dependent BT-474 (red) or rituximab-dependent Raji cell phagocytosis (green). MFI of PD-L1 (D) and IDO (E) in macrophages are as indicated.
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| S6846New |
Gly-Phe β-naphthylamideGly-Phe β-naphthylamide (Gly-Phe beta-naphthylamide)是在溶酶体内积累的组织蛋白酶 C 的底物。Gly-Phe-β-naphthylamide 可以抑制 caspase-8 的组织蛋白酶依赖性激活。 |
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| S9817New |
Ac-FLTD-CMKAc-FLTD-CMK 是一种特异性的 inflammatory caspases 的抑制剂。Ac-FLTD-CMK 在体外通过 caspases-1、-4、-5 和 -11 抑制 gasdermin D (GSDMD) 裂解。Ac-FLTD-CMK 对caspases-1、caspases-4 和 caspases-5 的IC50值分别为 46.7 nM、1.49 μM 和 329 nM。 |
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| S2417 |
20-Hydroxyecdysone20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone, Crustecdysone) 是一种自然发生的蜕皮激素，控制节肢动物的蜕皮和变态。20-Hydroxyecdysone (Ecdysterone, 20E) 可抑制 caspase 活性并通过20E核受体复合体 EcR-USP 来诱导自噬。 |
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| S7023 |
Z-VAD-FMKZ-VAD-FMK (Z-VAD(OMe)-FMK)是一种细胞渗透性的，不可逆泛caspase抑制剂，在THP.1 和 Jurkat T细胞中阻断细胞凋亡的所有特性。 |
(A and B) Western blot analysis examining the effect of zVAD-fmk on the icaritin-induced apoptosis. The caspase inhibitor zVAD-fmk could significantly decrease the icaritin-induced cleaved caspase-3 expression. β-Actin protein levels indicate that an equal amount of protein was loaded into each lane.n=3. Mean±SD. bP<0.05, compared to the control group. eP<0.05, compared to the icaritin-treated group. |
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| S7314 |
Z-IETD-FMKZ-IETD-FMK (Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK)是一种特异性Caspase-8抑制剂。 |
The caspase-8 inhibitors do not rescue NB4 cells from TPEN-triggered apoptosis. NB4 cells were pre-treated with 50 μM Z-ITED-FMK or 100 μM Ac-IETD-CHO for 1 h, and then treated with 5 μM TPEN for 24 h. (A) Cell morphology was observed and recorded using an optical microscope. The scale bar represents 20 μm. A partiallty enlarged view was shown in the lower left corner of every picture. (B) Apoptosis rate was measured with Annexin V/PI dual staining by flow cytometry.
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| S7313 |
Z-LEHD-FMK TFAZ-LEHD-FMK TFA (Caspase-9 Inhibitor) 是一种具有细胞透性、不可逆的Caspase-9抑制剂，有助于细胞生存。 |
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| S3267 |
Kaempferol-3-O-rutinosideKaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside) 是从 Carthamus tinctorius 中提取的黄酮，可改变受伤神经元的形状和结构，减少凋亡细胞，下调 p-JAK2、p-STAT3、caspase-3 和 Bax 的表达，并降低Bax免疫反应性，并增加 Bcl-2 蛋白表达和免疫反应性。 |
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| S7312 |
Z-DEVD-FMKZ-DEVD-FMK (Caspase-3 Inhibitor)是一种特异性，不可逆的Caspase-3抑制剂，也能有效抑制caspase-6， caspase-7， caspase-8和caspase-10。 |
(J,K)After pre-treated with Caspase-3 inhibitor Z-DEVD-FMK 50μM, the apoptotic rates of cells induced by E Platinum in BGC-823, MGC-803, and SGC-7901 cells were detected by Annexin V/PI double-staining assay. Ann.V-/PI- as healthy cells, Ann.+/PI- as early apoptotic cells, Ann.+/PI+ probably as late apoptotic cells. Data were shown as means SD for three independent experiments (*P<0.05 and **P<0.01 compared with control, ##P<0.01 compared to Z-DEVD-FMK+40 μM E Platinum group with treatment of 40 μM E Platinum). |
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| S7311 |
Q-VD-OphQ-VD-OPh (Quinoline-Val-Asp-Difluorophenoxymethylketone)是一种有效的pan-caspase抑制剂，作用于caspases 1， 3， 8和9，IC50范围在25到400 nM之间，有效抑制与细胞凋亡相关的末端caspase激活，底物裂解，及DNA梯状条带形成。Q-VD-OPh 可抑制HIV感染。 |
UA and Q-VD-Oph attenuated TNF-α-induced unclear translocation of NF-κB (C) and P-STAT3(S727) (D) in BEAS-2B cells.
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| S3275 |
Senkyunolide ISenkyunolide I (SEI, SENI) 是一种从 Ligusticum chuanxiong 中提取的口服活性化合物，具有止痛、抗偏头痛、神经保护、抗氧化和抗凋亡的活性。Senkyunolide I (SEI, SENI) 可上调 Erk1/2 的磷酸化，并诱导 Nrf2 的核易位，伴随着HO-1和NQO1的表达增强。Senkyunolide I (SEI, SENI) 可提高 Bcl-2/Bax 的比例，并抑制裂化的 caspase 3 和 caspase 9 的表达。 |
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| S8507 |
Z-YVAD-FMKZ-YVAD-FMK 是一种具有抗炎和抗肿瘤活性的细胞渗透性的、不可逆的 caspase-1 特异性抑制剂。 |
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| S8102 |
Z-VAD(OH)-FMK (Caspase Inhibitor VI)Z-VAD(OH)-FMK (Caspase Inhibitor VI) 是一类不可逆的泛caspase抑制剂。 |
Effect on the RAS of CFZ, z-VAD-fmk, or CFZ+z-VAD-fmk treatments administered 5 or 12 days after C26 inoculation and control groups. Serum levels of a renin and b ANGII. c The mRNA expression of ATF2. d Western blot analysis of ATF2 and pATF2. e pATF2-to-ATF2 ratio. Significant differences were detected between most of the groups, with the exceptionsof (A and B) CP and UT (D) and ZP and ZT (#); and (C and E) CP and UP (*), CT and UT (#), and HC, ZP, ZT and CC (&). ZP:z-VAD-fmk.
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| S7775 |
Emricasan (IDN-6556)Emricasan (IDN-6556, PF 03491390, PF-03491390)是有效的、不可逆的泛半胱天冬酶（pan-caspase）抑制剂。Emricasan 也是寨卡病毒感染的抑制剂。 |
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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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| S9075 |
Mulberroside AMulberroside 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-α、IL-1β 和 IL-6 的表达并抑制 NALP3、caspase-1 和 NF-κB 的激活以及 ERK、JNK 和 p38 的磷酸化。 |
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| S7901 |
Ac-DEVD-CHOAc-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO)是Group II caspases的有效抑制剂，对caspase-3和caspase-7的Ki值分别为0.2 nM和1.6 nM。对caspase-2制剂效果弱，Ki值为1.7 μM。 |
Microwave (MW) hyperthermia triggers cell death through caspase-3-mediated apoptosis. H460, PC-9 and H1975 cells were treated with or without Ac-DEVD-CHO for 3 h prior to MW hyperthermia (43°C for 90 min), then allowed to recover at 37°C until 24 h. (A) Cell viability was determined by CCK-8 assay. Data are expressed as the means ± SEM of 3 independent experiments. *P<0.05 vs. the control group, **P<0.01 vs. the control group.
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| S5579 |
Chelidonic acidChelidonic 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-κB 和 caspase-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。 |
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| S5584 |
CitronellolCitronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1029 |
Lenalidomide (CC-5013)Lenalidomide (CC-5013)是一种TNF-α分泌抑制剂，在PBMCs中IC50为13 nM。Lenalidomide (CC-5013) 是 ubiquitin E3 ligase cereblon (CRBN) 的配体，它通过CRBN-CRL4泛素连接酶引起两个淋巴样转录因子IKZF1和IKZF3的选择性泛素化和降解。Lenalidomide 可促进 cleaved caspase-3 的表达、抑制 VEGF 的表达并诱导凋亡。 |
Effect of lenalidomide treatment (50 mg/kg/day, p.o. for 3 days) on expression of tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), Fas, Fas ligand (FasL), and cleaved caspase-3 in myocardium from lean and ob/ob mice. (a) Representative gel blots of TNF-α, IL-6, Fas, FasL, cleaved caspase-3 and α-Tubulin (as loading control) using specific antibodies. (b) TNF-α. |
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| S2768 |
Dinaciclib (SCH727965)Dinaciclib (SCH727965, PS-095760) 是一种新型有效的CDK抑制剂，作用于CDK2，CDK5，CDK1和CDK9，无细胞试验中IC50分别为1 nM，1 nM，3 nM和4 nM。它也会阻断胸甘(dThd) DNA整合。Dinaciclib 可通过激活caspases 8和caspases 9来诱导细胞凋亡。Phase 3。 |
CDK4/6 inhibition has potent cytostatic effect in HER2-positive models. The indicated cells were treated with PD-0332991 (1 uM) or Dinaciclib (1 uM) for 96 hours and plates were stained with crystal violet.
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| S2738 |
PAC-1PAC-1是一种有效的procaspase-3（酶原-3）激活剂，EC50为0.22 μM，是第一个已知的直接激活酶原e-3为caspase-3的小分子。 |
The effects of PAC-1 (activator of ROS) administration on the newborn pups' weight and the plasma IGF-1 and ROS levels in graviditas gp91phox-/- mice. The values are presented as the means ± SD derived from six animals. *P<0.05 in comparison to the non-treatment mice.
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| S2891 |
GW441756GW441756 是一种有效的，选择性的TrkA抑制剂，IC50为2 nM，对c-Raf1和CDK2几乎没有抑制活性。GW441756 可增加caspase-3并诱导凋亡。 |
Thermal latency and mechanical allodynia were normalized in the RTXw1 + 4MC group (n= 6). In these mice, thermal hypoalgesia reappeared within 2 days of GW441756 injection (D). GW441756 did not affect mechanical thresholds (E) in the RTXw1 + 4MC group. (F, G) The diagrams show behavioral responses of naïve mice to either gambogic amide (open square, n = 6) or GW441756 (open circle, n =6). Gambogic amide induced mild thermal hyperalgesia within 2 days of injection but GW441756 did not affect thermal latencies (F). Both gambogic amide and GW441756 did not affect mechanical responses. *P < 0.05, **P < 0.01, and ***P < 0.001: paired t-test comparing preinjection vs. postinjection effects. #P < 0.05, ##P < 0.01, and ###P < 0.001: between drugs and saline treatments.
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| S2927 |
Apoptosis Activator 2Apoptosis Activator 2强诱导caspase-3激活， PARP分裂， DNA断裂，导致细胞破坏(Apaf-1依赖性的)，IC50约为4 μM，抑制HMEC， PREC和MCF-10A细胞活性。 |
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| S7326 |
TasisulamTasisulam (LY573636)是一种抗肿瘤剂，是通过内源途径导致细胞凋亡的诱导物。 Phase 3 |
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| S6899 |
Licochalcone DLicochalcone 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 JAK2、EGFR 和 Met (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。 |
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| S0913 |
4',5,7-Trimethoxyflavone4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) 是一种从 Kaempferia parviflora (KP) 分离的类黄酮，可诱导凋亡。4',5,7-Trimethoxyflavone 可增加亚G1期、DNA片段化、膜联蛋白-V/PI染色和Bax/Bcl-xL比，激活 caspase-3 并降解 poly (ADP-ribose) polymerase (PARP) 蛋白。 |
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| S6501 |
NVP 231NVP 231是新型CerK抑制剂，在体外抑制重组CerK的催化活性，IC50为12 nM。 |
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| S3238 |
ResibufogeninResibufogenin (Bufogenin, Recibufogenin) 是huachansu华蟾素中具有抗癌作用的成分，通过上调 receptor-interacting protein kinase 3 (RIP3) 和磷酸化 mixed lineage kinase domain-like protein 的Ser358位点来触发坏死病。Resibufogenin 可通过诱导 reactive oxygen species (ROS) 积累发挥细胞毒性作用。Resibufogenin 可诱导凋亡和 caspase-3 和 caspase-8 活性。Resibufogenin 增加 Bax/Bcl-2 表达，并抑制 cyclin D1、cyclin E、PI3K、p-AKT、p-GSK3β 和 β-catenin 的蛋白表达。 |
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| S9276 |
Alisol BAlisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways. |
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| S2271 |
Berberine chloride (NSC 646666)Berberine chloride (NSC 646666, Natural Yellow 18)是异喹啉类生物碱的季铵盐。Berberine chloride 可激活 caspase 3 和 caspase 8，分裂 poly ADP-ribose polymerase (PARP) 和释放 cytochrome c。Berberine chloride 可降低 c-IAP1，Bcl-2 和 Bcl-XL 的表达。Berberine chloride 可通过 JNK 和 p38 MAPK 的持续磷酸化以及产生 ROS 来诱导凋亡。Berberine chloride 是一个 topoisomerase I 和 II 的双效抑制剂。Berberine chloride 也是一个潜在的自噬调节剂。 |
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| S2448 |
Gambogic AcidGambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin)激活caspases，EC50为0.78 - 1.64 μM，且完全抑制Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 和 Mcl-1，IC50分别为1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM 和 0.79 μM。 |
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| S5967 |
Berberine chloride hydrateBerberine (Natural Yellow 18) chloride hydrate 是属于异喹啉生物碱的季铵盐。Berberine 可激活 caspase 3 和 caspase 8，poly ADP-ribose polymerase (PARP) 的切割和 cytochrome c 的释放。Berberine chloride 可降低 c-IAP1、Bcl-2 和 Bcl-XL 的表达。Berberine chloride 通过 JNK 和 p38 MAPK 的持续磷酸化以及 ROS的生成来诱导凋亡。Berberine chloride 是一种 topoisomerase I 和 II 的双重抑制剂。Berberine chloride 也是一种潜在的自噬调节剂。 |
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| S0354 |
AlsterpaulloneAlsterpaullone (Alp, 9-Nitropaullone, NSC 705701) 是一种 CDK 的有效抑制剂，对CDK1/cyclin B、CDK2/cyclin A、CDK2/cyclin E 和 CDK5/p35的IC50值分别为35 nM、15 nM、200 nM和40 nM。Alsterpaullone 还可作为 glycogen synthase kinase-3 (GSK-3) 的有效抑制剂，对GSK-3α和GSK-3β的IC50值均为4 nM。Alsterpaullone 可通过激活 caspase-9 诱导凋亡。Alsterpaullone 具有抗肿瘤活性，具有治疗神经退行性和增生性疾病的潜力。 |
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| S4513 |
RGD peptide (GRGDNP)RGD peptide (GRGDNP) 是 integrins 与细胞外基质结合的抑制剂。RGD peptide (GRGDNP) 可能通过直接激活 caspase-3 并诱导凋亡。 |
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| S9097 |
Alisol B AcetateAlisol B acetate, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways. |
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| S5550 |
Ethyl gallateEthyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity. |
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| S6990 |
PhytohemagglutininPhytohemagglutinin (PHA, Phaseolus vulgaris agglutinin) 在毕赤酵母中利用天然信号肽或酿酒酵母α-因子前体序列表达，将蛋白质引导至分泌途径。Phytohemagglutinin 可通过增加凋亡蛋白 Bax 和激活 caspases-3 来诱导人HEp-2癌细胞的凋亡。 |
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| S9634 |
Phenoxodiol (Haginin E)Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) 是一种具有抗肿瘤活性的异黄酮类似物，可激活 caspase 系统，抑制 XIAP (X-linked inhibitor of apoptosis)，并破坏 FLICE inhibitory protein (FLIP) 的表达，从而导致肿瘤细胞凋亡。Phenoxodiol 也抑制 DNA topoisomerase II。 |
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| S4353 |
TerfenadineTerfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9. |
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| S3865 |
Taurochenodeoxycholic acidTaurochenodeoxycholic acid (Taurochenodeoxycholic acid (Taurochenodeoxycholate, TCDCA, Chenodeoxycholyltaurine)), a bile acid formed in the liver of most species, is used as a cholagogue and choleretic. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S3224 |
CinobufaginCinobufagin (Cinobufagine) 是 Venenum Bufonis 的活性成分，可抑制肿瘤发展。Cinobufagin 可提高 ATM 和 Chk2 并降低 CDC25C、CDK1 和 cyclin B。Cinobufagin 抑制 PI3K、AKT 和 Bcl-2，同时增加裂解的 caspase-9 和 caspase-3 水平。由此诱导细胞周期停滞在G2/M期及凋亡。 |
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| S6882 |
HI-TOPK-032HI-TOPK-032 是一种有效的、特异性的 TOPK 的抑制剂。HI-TOPK-032 还可以降低 ERK-RSK 磷酸化，调节 p53、裂化的 caspase-7 和裂化的 PARP 的丰度，并在癌细胞中诱导凋亡。 |
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| S3088 |
(±)-Methyl Jasmonate(±)-Methyl Jasmonate (MeJA, Methyl jasmonate, Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate)，是一种植物激素，在植物中起着至关重要的细胞调节剂的作用，是调节炎症性肠病(IBDs)的新候选药物，可调节 caspase 型蛋白酶家族主要类型的表达。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8487New |
AP20187AP20187 (B/B Homodimerizer, HY-13992) 是一种二聚化的化学诱导剂，可激活 FKBP-Casp8。 |
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