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MilliporeSigma™ Calbiochem™ PERK Inhibitor II, GSK2656157

Catalog No. 5046510001 Shop All MilliporeSigma Products
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50-465-10001 5 mg
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Catalog No. 50-465-10001 Supplier MilliporeSigma™ Supplier No. 5046510001
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Description

PERK Inhibitor II, GSK2656157, CAS 1337532-29-2 is a cell-permeable, potent, ATP-competitive inhibitor of PERK/EIF2AK3 (IC50 = 0.9nM).

A cell-permeable pyrrolopyrimidinamine compound that acts as a potent, ATP-competitive EIF2AK3/PERK inhibitor (IC50 = 0.9nM; [ATP] = 10μM), displaying ≥511-fold selectivity over HRI/EIF2AK1, BRK, PKR/EIF2AK2, and MEKK2 (IC50 = 460, 822, 905, and 954 nM, respectively) and much reduced or little activity toward more than 300 other kinases. Potently prevents ER stress-induced enhancement of PERK and eIF2α phosphorylation as well as ATF4 and CHOP upregulation in human BxPC3 and murine LL/2 cultures in vitro (IC50 ≤30nM; 1 h drug preincubation prior to 6 h 1μM Thapsigargin treatment, Cat. No. 586005) and exhibits antitumor efficacy against 3 pancreas and 1 multiple myeloma xenografts in mice (54-110% tumor growth inhibition; 150mg/kg/12 h via p.o.) in vivo . More selective than GSK2606414 (Cat. No. 516535).
TRUSTED_SUSTAINABILITY

Specifications

Color White
Description 98% by HPLC
Target Proteins PERK
Molecular Formula C23H21FN6O
Solubility DMSO
Content And Storage Protect from light
Form Powder
Quantity 5 mg
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