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GSK2656157

Catalog No. T2654 CAS 1337532-29-2

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.

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GSK2656157, CAS 1337532-29-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 32.00
5 mg	In stock	$ 51.00
10 mg	In stock	$ 74.00
25 mg	In stock	$ 145.00
50 mg	In stock	$ 272.00
100 mg	In stock	$ 492.00
200 mg	In stock	$ 665.00
1 mL * 10 mM (in DMSO)	In stock	$ 81.00

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Purity: 100%

Purity: 99.89%

Purity: 97.77%

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Storage & Solubility Information

Description	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.
Targets&IC50	PERK:0.9 nM
In vitro	GSK2656157 inhibits the growth of various human xenograft tumors in mice. Administered at a dose of 50 mg/kg orally, GSK2656157 completely suppresses phospho-PERK Thr980 after 8 hours. Furthermore, with dosages of 50/150 mg/kg administered twice daily, GSK2656157 exhibits a dose-dependent suppression of tumor growth in four different mouse cancer models, achieving a 54-114% inhibition of tumor growth at 150 mg/kg.
In vivo	GSK2656157 (1 mM) can induce the unfolded protein response (UPR) and inhibit de novo protein synthesis. It downregulates 6% of UPR-related genes (PPP1R15A, HERPUD1, DDIT3, C/EBP-β, and ERN1), with a reduction exceeding fourfold for these targets. Pre-treatment with GSK2656157 inhibits PERK activation and decreases downstream substrates, including phospho-eIF2a, ATF4, and CHOP (IC50: 10-30 nM). In the absence of exogenous UPR inducers, GSK2656157 does not affect cell growth (IC50: 6-25 mM).
Kinase Assay	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.
Cell Research	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)

Molecular Weight	416.45
Formula	C23H21FN6O
CAS No.	1337532-29-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

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

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

DMSO: 30 mg/mL (72 mM)

References and Literature

1. Atkins C, et al. Cancer Res, 2013, 73(6), 1993-2002.

Citations

1. Tan M, Wang H, Gao C, et al. Agonists Specific for κ-Opioid Receptor Induces Apoptosis of HCC Cells Through Enhanced Endoplasmic Reticulum Stress. Frontiers in Oncology. 2022.12 2. Lu Y, Li D, Ai H, et al.Glucose-regulated protein 94 facilitates the proliferation of the Bombyx mori nucleopolyhedrovirus via inhibiting apoptosis.International Journal of Biological Macromolecules.2023: 127158.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Highly Selective Inhibitor Library Target-Focused Phenotypic Screening Library Anti-Obesity Compound Library HIF-1 Signaling Pathway Compound Library Neural Regeneration Compound Library Anti-Aging Compound Library Apoptosis Compound Library Reprogramming Compound Library

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Keywords

GSK2656157 1337532-29-2 Apoptosis Autophagy PERK PKR-like endoplasmic reticulum kinase GSK 2656157 Protein kinase R-like endoplasmic reticulum kinase Inhibitor GSK-2656157 inhibit inhibitor

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