Name: GSK2656157
Price: 258.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    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].
    
    [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.
- Properties
  - Alternative Name
    
    1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethanone
    
    CAS Number
    
    1337532-29-2
    
    Molecular Formula
    
    C23H21FN6O
    
    Molecular Weight
    
    416.45
    
    Appearance
    
    A solid
    
    Purity
    
    99.33%
    
    Solubility
    
    insoluble in H2O; ≥2.5 mg/mL in EtOH with gentle warming and ultrasonic; ≥20.82 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Luo J, Xia Y, et al. "GRP78 inhibition enhances ATF4-induced cell death by the deubiquitination and stabilization of CHOP in human osteosarcoma." Cancer Lett. 2017 Sep 22. pii:S0304-3835(17)30571-2. PMID:28947141
    2. Rojas-Rivera D, Delvaeye T, et al. "When PERK inhibitors turn out to be new potent RIPK1 inhibitors:critical issues on the specificity and use of GSK2606414 and GSK2656157." Cell Death Differ. 2017 Jun;24(6):1100-1110. PMID:28452996

GSK2656157

GSK2656157

Background

We Also Recommend

BAY 80-6946 (Copanlisib)

GSK1059615

TG100713