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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PERK-GSK-2656157
GSK-2656157

Chemical Structure : GSK-2656157

CAS No.: 1337532-29-2

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GSK-2656157 (GSK2656157)

货号: PC-49643Not For Human Use, Lab Use Only.

GSK2656157 (GSK 2656157) is a potent, selective and ATP-competitive inhibitor of PERK with biochemical IC50 of 0.9 nM and cellular p-PERK IC50 of 30 nM.

规格 价格 库存 数量
5 mg ￥580 In stock
10 mg ￥980 In stock
25 mg ￥1580 In stock
50 mg ￥2380 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK2656157 (GSK 2656157) is a potent, selective and ATP-competitive inhibitor of PERK with biochemical IC50 of 0.9 nM and cellular p-PERK IC50 of 30 nM.
GSK2656157 shows selectivity (>500-fold) over HRI, PKR, and GCN2, other members of the EIF2AK family, and high IC50 values (>100 nM) against a panel of 300 kinases.
GSK2656157 inhibits stress-induced PERK autophosphorylation, eIF2α substrate phosphorylation, together with corresponding decreases in ATF4 and CAAT/enhancer binding protein homologous protein (CHOP) in multiple cell lines.
Oral administration of GSK2656157 to mice shows a dose- and time-dependent pharmacodynamic response in pancreas as measured by PERK autophosphorylation.
GSK2656157 exhibited antitumor effect in multiple human tumor xenografts growth in mice.

物理化学性质&存储条件

分子量 416.45
分子式 C23H21FN6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydro-1H-indol-1-yl]-2-(6-methyl-2-pyridinyl)ethanone

参考文献

1. Atkins C, et al. Cancer Res. 2013 Mar 15;73(6):1993-2002.

2. Krishnamoorthy J, et al. Cell Cycle. 2014;13(5):801-6.

3. Axten JM, et al. ACS Med Chem Lett. 2013 Aug 12;4(10):964-8.

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