GSK2656157
货号：
17372-5mg 基本售价：
490.0 元 规格：
5 mg
产品信息
概述| 货号 | 17372-5mg |
| 描述 | GSK2656157 is an inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK; IC50 = 0.9 nM).1,2 It is selective for PERK over a panel of additional kinases.1 GSK2656157 blocks both stress-induced PERK autophosphorylation and eIF2α substrate phosphorylation and decreases levels of ATF4 and CHOP in multiple cell lines.1 It is orally bioavailable, suppressing PERK autophosphorylation in mouse pancreas and inhibiting the growth of multiple human tumor xenografts in mice.1,2 GSK2656157 inhibits caspase 1 activation in macrophage-like J774.1 cells, preventing LPS-induced IL-1β production, through its effects on the PERK/eIF2α pathway.3 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Atkins, C.,Liu, Q.,Minthorn, E., et al. Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 73(6), 1993-2002 (2013).
2.Axten, J.M.,Romeril, S.P.,Shu, A., et al. Discovery of GSK2656157: An optimized PERK inhibitor selected for preclinical development. ACS Med. Chem. Lett. 4, 964-968 (2013).
3.Ando, T.,Komatsu, T.,Naiki, Y., et al. GSK2656157, a PERK inhibitor, reduced LPIS-induced IL-1b production through inhibiting caspase 1 activation in macrophage-like J774.1 cells. Immunopharmacol. Immunotoxicol. 38(4), 298-302 (2016).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 416.5 |
| 分子式 | C23H21FN6O |
| CAS号 | 1337532-29-2 |
| 稳定性 | ≥ 2 years |
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