Name: GSK2656157
Brand: TargetMol
SKU: T2654
Price: 278 CNY
Availability: InStock
Rating: 5 (10 reviews)

规格

价格

库存

数量

1 mg

¥ 278

In stock

2 mg

¥ 393

In stock

5 mg

¥ 579

In stock

10 mg

¥ 967

In stock

25 mg

¥ 1,520

In stock

50 mg

¥ 2,090

In stock

100 mg

¥ 3,480

In stock

200 mg

¥ 4,960

In stock

1 mL x 10 mM (in DMSO)

¥ 637

In stock

产品介绍

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	BRK:905 nM, ROCK1:7244 nM, PERK:0.9 nM, LRRK2:6918 nM, NEK1:9807 nM, MLCK2:3039 nM, EIF2AK1 (HRI):460 nM, KHS:1764 nM, EIF2AK4(GCN2):3162 nM, WNK3:5951 nM, PI3Kγ:3802 nM, ALK5:3020 nM, EIF2AK2 (PKR):905 nM, MLK2:2796 nM, JAK2:24547 nM, AXL:9808 nM, Aurora B:1259 nM, MEKK3:954 nM, c-MER:3431 nM, MSK1:8985 nM, LCK:2344 nM, MEKK3:2847 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: 30 mg/mL (72.04 mM), Sonication is recommended.

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
50 mM	0.0480 mL	0.2401 mL	0.4802 mL	2.4012 mL

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是 10 mg/kg ，每只动物体重 20 g ，给药体积 100 μL ， TargetMol | Animal experiments

一共给药动物 10 只 ，您使用的配方为 5% TargetMol | reagent

DMSO+ 30%PEG300+ 5%Tween 80 + 60%Saline/PBS/ddH₂O，那么您的工作液浓度为 2 mg/mL 。

母液配置方法: 2 mg 药物溶于 50 μLDMSO TargetMol | reagent

（母液浓度为 40 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法: 取 50μLDMSO TargetMol | reagent

母液，添加 300 μLPEG300 TargetMol | reagent

混匀澄清，再加 50μLTween 80, 混匀澄清，再加 600μLSaline/PBS/ddH₂O TargetMol | reagent

混匀澄清

以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如： DMSO， PEG300/ PEG400， Tween 80， SBE-β-CD，玉米油等，均可在TargetMol网站点击购买。

GSK2656157

GSK2656157

产品介绍

计算器

体内实验配液计算器

剂量转换

SCI 文献

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