规格

价格

库存

数量

1 mg

¥ 278

现货

2 mg

¥ 393

现货

5 mg

¥ 579

现货

10 mg

¥ 967

现货

25 mg

¥ 1,520

现货

50 mg

¥ 2,090

现货

100 mg

¥ 3,480

现货

200 mg

¥ 4,960

现货

1 mL x 10 mM (in DMSO)

¥ 637

现货

生物活性

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	EIF2AK4(GCN2):3162 nM, LRRK2:6918 nM, NEK1:9807 nM, MLK2:2796 nM, EIF2AK1 (HRI):460 nM, AXL:9808 nM, PI3Kγ:3802 nM, KHS:1764 nM, JAK2:24547 nM, PERK:0.9 nM, MEKK3:954 nM, MEKK3:2847 nM, MLCK2:3039 nM, MSK1:8985 nM, Aurora B:1259 nM, ROCK1:7244 nM, LCK:2344 nM, c-MER:3431 nM, WNK3:5951 nM, ALK5:3020 nM, BRK:905 nM, EIF2AK2 (PKR):905 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)

化学信息

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)

储存&溶解度

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 13.89 mg/mL (33.35 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 0.5 mg/mL (1.2 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4012 mL	12.0062 mL	24.0125 mL	120.0624 mL
5 mM	0.4802 mL	2.4012 mL	4.8025 mL	24.0125 mL
10 mM	0.2401 mL	1.2006 mL	2.4012 mL	12.0062 mL
20 mM	0.1201 mL	0.6003 mL	1.2006 mL	6.0031 mL