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GSK2656157 是一种ATP 竞争性的PERK 选择性抑制剂,IC50值为 0.9 nM。
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GSK2656157 是一种ATP 竞争性的PERK 选择性抑制剂,IC50值为 0.9 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 278 | 现货 | |
2 mg | ¥ 393 | 现货 | |
5 mg | ¥ 659 | 现货 | |
10 mg | ¥ 967 | 现货 | |
25 mg | ¥ 1,560 | 现货 | |
50 mg | ¥ 2,120 | 现货 | |
100 mg | ¥ 3,870 | 期货 | |
200 mg | ¥ 5,490 | 期货 | |
1 mL x 10 mM (in DMSO) | ¥ 795 | 现货 |
产品描述 | GSK2656157 is a highly specific and ATP-competitive PERK inhibitor (IC50: 0.9 nM) in a cell-free assay. The selectivty is 500-fold higher against a panel of 300 kinases. |
靶点活性 | PERK:0.9 nM |
体外活性 | GSK2656157可抑制小鼠体内多种人移植瘤生长.GSK2656157(50 mg/kg,p.o.)处理8 h后,完全抑制phospho-PERK Thr980. GSK2656157(50/150 mg/kg,2次/天)剂量依赖性地抑制小鼠体内四种肿瘤模型生长,150 mg/kg可抑制54-114%肿瘤生长. |
体内活性 | GSK2656157(1 mM)可进行UPR诱导,并抑制de novo蛋白合成。GSK2656157下调6%的UPR相关基因(PPP1R15A,HERPUD1,DDIT3,C/EBP-β和ERN1),且有超过4倍的下调。GSK2656157预处理细胞可抑制PERK活化,且可使下游底物、phospho-eIF2a、ATF4和 CHOP减少(IC50:10-30 nM)。在无外源UPR诱导剂时,GSK2656157则不影响这些细胞的生长(IC50:6-25 mM)。 |
激酶实验 | Kinase assay: Inhibitory potency of GSK2656157 is measured using recombinant GST-PERK (536–1116 amino acids) with 6-His-full-length human eIF2a as a substrate. Kinase selectivity is evaluated using 27 kinases at GSK as well as a panel of 300 kinases. |
细胞实验 | Antiproliferative activity of GSK2656157 against multiple human tumor cell lines as well as primary human microvascular endothelial cells is evaluated in a 3-day proliferation assay using standard culture medium. In the absence of exogeneous UPR inducers, GSK2656157 has no significant effect on the growth of any of these cells with IC50 range of 6–25 mM. (Only for Reference) |
分子量 | 416.45 |
分子式 | C23H21FN6O |
CAS No. | 1337532-29-2 |
Smiles | Cc1cccc(CC(=O)N2CCc3c2ccc(-c2cn(C)c4ncnc(N)c24)c3F)n1 |
密度 | 1.43 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 30 mg/mL (72 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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