GSK2656157, PERK inhibitor

Product Details

Formal Name: 1-[5-(4-Amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydroindol-1-yl]-2-(6-methylpyridin-2-yl)ethanone

Molecular Formula: C₂₃H₂₁FN₆O

Formula Weight: 416.50

CAS Number: 1337532-29-2

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 10 mg/ml with warming)

Storage: -20°C

Stability: ≥ 1 year.

Applications

PERK inhibitor

Functions

Potent (IC50 = 0.9 nM) and selective (over 300 kinases) inhibitor of protein kinase RNA-like endoplasmic reticulum kinase (PERK). Inhibited growth of multiple human tumor xenografts in mice. Also potently inhibits RIPK1 (IC50 = 69 nM) and TNF-mediated RIPK1 kinase-dependent cell death in MEFs. Prevented the loss of dendritic spines and rescued memory deficits after traumatic brain injury. Enhances glucose-stimulated insulin secretion in a mouse model of type 2 diabetes mellitus.

Application Procedures

First dissolved in DMSO (up to 10 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 1 month.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)