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GSK2656157 Sale

目录号 : GC11068

A PERK inhibitor

GSK2656157 Chemical Structure

Cas No.:1337532-29-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,145.00
现货
10mg
¥893.00
现货
50mg
¥1,953.00
现货
100mg
¥3,539.00
现货

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment [1]:

Cell lines

HT1080 cells

Preparation method

The solubility of this compound in DMSO is > 20.8 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.1-10 µM, 24 h

Applications

In HT1080 cells, 0.1 μM GSK2656157 was efficient to block the activity of PERK. Cells treated with GSK2656157 exhibited increasing eIF2α phosphorylation in order to compensating the loss of PERK.

Animal experiment [2]:

Animal models

Eight- to twelve-week-old naive female CD-1, female nu/nu CD-1 mice and severe combined immunodeficient (SCID) mice

Dosage form

50, 150 mg/kg, twice daily

Application

After a single 50 mg/kg oral dose of GSK2656157, mice occurs inhibited phospho-PERK in the pancreas completely through 8 hours. And the activity of PERK was recovered to almost normal levels at 18 hours. Twice daily administration of 50 or 150 mg/kg GSK2656157 to mice resulted in an inhibition of multiple tumor xenografts growth in a dose-dependent manner.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Krishnamoorthy J, Rajesh K, Mirzajani F, et al. Evidence for eIF2α phosphorylation-independent effects of GSK2656157, a novel catalytic inhibitor of PERK with clinical implications[J]. Cell Cycle, 2014, 13(5): 801-806.

[2]. Atkins C, Liu Q, Minthorn E, et al. Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity[J]. Cancer research, 2013, 73(6): 1993-2002.

产品描述

GSK2656157 is a highly selective inhibitor of protein kinase R-like ER kinase (PERK) with IC50 value of 0.9nM [1].

GSK2656157 is highly selective for PERK enzyme against a panel of 300 kinases. In the BxPC3 pancreatic tumor cell line, treatment of GSK2656157 causes an inhibition of PERK and decreases in the downstream substrates, including phospho-eIF2α, ATF4 and CHOP. The inhibition of PERK results in effects on de novo protein synthesis as shown in BxPC3 cells [1].

In vivo assay shows that a single 50 mg/kg oral dose of GSK2656157 can completely inhibit the Thr980 phosphorylation of endogenous pancreatic PERK in mice. Furthermore, GSK2656157 causes dose-dependent inhibition of tumor growth in human tumor xenograft models of pancreatic cancer (BxPC3, HPAC and Capan2) and multiple myeloma (NCI-H929). Among these cancers, the Capan2 tumor is most sensitive [1].

References:
[1] Atkins C, Liu Q, Minthorn E, Zhang SY, Figueroa DJ, Moss K, Stanley TB, Sanders B, Goetz A, Gaul N, Choudhry AE, Alsaid H, Jucker BM, Axten JM, Kumar R. Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 2013 Mar 15;73(6):1993-2002.

Chemical Properties

Cas No. 1337532-29-2 SDF
化学名 1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethanone
Canonical SMILES NC1=NC=NC2=C1C(C3=CC=C4C(CCN4C(CC5=NC(C)=CC=C5)=O)=C3F)=CN2C
分子式 C23H21FN6O 分子量 416.45
溶解度 ≥ 20.8225mg/mL in DMSO 储存条件 Store at -20° C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.4012 mL 12.0062 mL 24.0125 mL
5 mM 0.4802 mL 2.4012 mL 4.8025 mL
10 mM 0.2401 mL 1.2006 mL 2.4012 mL
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