IAP
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S7597 | BV-6 | 25 mg/mL | 100 mg/mL | 100 mg/mL |
| S7362 | AZD5582 | 100 mg/mL | -1 mg/mL | -1 mg/mL |
| S7025 | Embelin | <1 mg/mL | 59 mg/mL | 12 mg/mL |
| S7009 | LCL161 | <1 mg/mL | 100 mg/mL | 20 mg/mL |
| S7015 | Birinapant | <1 mg/mL | 100 mg/mL | 55 mg/mL |
| S7010 | GDC-0152 | 3 mg/mL | 99 mg/mL | 99 mg/mL |
| S2754 | AT406 (SM-406) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
特异性亚型抑制剂
- IAP抑制剂（7）
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7597 |
BV-6BV-6是一种SMAC模拟的cIAP和XIAP的双重抑制剂。 |
IEC-1 cells were transfected with Per1/2 specific siRNAs or a control siRNA. Afterward, the cells were stimulated with TNFa (0.1 ng/ml under basal conditions) in the presence or absence of BV-6 or were left untreated. Activation of caspase-8 (I) and caspases 3/7 (J ) was assayed. Data are presented as the means±SEM of at least 3 independent experiments. *P≤0.05, **P≤0.01. |
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| S7362 |
AZD5582AZD5582，一种新型的小分子IAP抑制剂，与cIAP1, cIAP2和XIAP的BIR3区域有效结合，IC50分别为15, 21, 15 nM。 |
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| S7025 |
EmbelinEmbelin，从矮地茶中分离的一种醌类化合物，是一种细胞凋亡的X染色体抑止剂(XIAP)的抑制剂，无细胞试验中IC50为4.1 μM。 |
(d) Representative plots of apoptosis in Jurkat cells treated with vehicle only, BIO, CN585, Embelin (Emb), BIO plus CN585 or BIO plus CN585 plus Emb.
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| S7009 |
LCL161LCL-161, 一种second mitochondrial activator of caspase (SMAC, 线粒体促凋亡蛋白)模拟物, 能有效地结合并抑制多种IAPs(i.e. XIAP, c-IAP)。 |
The Smac mimetic LCL-161, which inhibits cIAP1, modestly sensitizes hair cells to gentamicin damage. (A) Variable LCL-161 concentrations do not affect toxicity to 50 μM neomycin (one-way ANOVA, F4,69 = 1.54, p = 0.199). (B) Variable LCL has a modest but significant effect on gentamicin toxicity (one-way ANOVA, F4,31 = 3.14, p = 0.028), with 10 μM LCL conveying significant sensitization (∗p < 0.05).
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| S7015 |
BirinapantBirinapant是一种SMAC模拟拮抗剂，对cIAP1最有效，无细胞试验中Kd为<1 nM，对XIAP作用较弱。Phase 2。 |
Western blot from tumours harvested at day 5 after treatment showing an increase in PARP cleavage in the irinotecan-treated group.
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| S7010 |
GDC-0152GDC-0152是一种有效的XIAP-BIR3，ML-IAP-BIR3，cIAP1-BIR3和cIAP2-BIR3拮抗剂，无细胞试验中Ki分别为28 nM，14 nM，17 nM和43 nM，对cIAP1-BIR2和cIAP2-BIR2具较低亲和力。Phase 1。 |
(a) Apoptosis (SubG0/G1) of DMSO control and GDC-0152-treated cells was determined by flow cytometry of propidium iodide-stained nuclei and percentage of apoptosis is shown. U87MG and GL261 cell lines were treated for 72 h and GBM6 and GBM9 cell lines were treated for 8 days at the indicated concentrations. At these respective time points, percentage of U87MG cells dead by apoptosis, percentage of GL261 cells, percentage of GBM6 cells and percentage of GBM9 cells. Data are expressed as mean+S.E.M. Three independent experiments were performed for the GL261 cell lines and five for the U87MG, GBM6 and GBM9 cell lines. *P<0.05; **P<0.01; ***P<0.005.
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| S2754 |
AT406 (SM-406)AT-406是一种有效的，拟Smac的IAP(通过E3泛素连接酶起作用的凋亡蛋白抑制剂)拮抗剂，与XIAP-BIR3， cIAP1-BIR3和cIAP2-BIR3结合，Ki为66.4 nM， 1.9 nM和5.1 nM，比作用于Smac AVPI肽亲和力高50到100倍。Phase 1。 |
G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting. |
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