GSK2656157
作者：齐岳
发布时间：2023-09-13
17:03:40
点击数：
产品名称：GSK2656157
产品描述：
| 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 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
Ethanol: <1 mg/mL
DMSO: 30 mg/mL (72 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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