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MilliporeSigma™ Calbiochem™ InSolution™ PERK Inhibitor I, GSK2606414

Catalog No. 5083400001
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Quantity:
2 mg

A cell-permeable pyrrolopyrimidinamine compound that acts as a highly potent inhibitor against EIF2AK3/PERK-catalyzed EIF2α Ser51 phosphorylation in kinase assays (IC50 = 0

A cell-permeable pyrrolopyrimidinamine compound that acts as a highly potent inhibitor against EIF2AK3/PERK-catalyzed EIF2α Ser51 phosphorylation in kinase assays (IC50 = 0.4nM; 30 min preincubation; [ATP] = 5μM) as well as ER stress-induced PERK autophosphorylation following Thapsigargin (Cat. No. 586005) addition in A549 cultures (by 100% with ≤30nM inhibitor; 60 min preincubation) by targeting PERK in its inactive conformation at the ATP-binding region. Displays ≥385-fold selectivity over c-Kit, Aurora B, BRK, HRI/EIF2AK1, MLK2/MAP3K10, c-MER, DDR2, PKR/EIF2AK2, and MLCK2/MYLK2 (IC50 = 154, 407, 412, 420, 452, 474, 524, 696, and 701 nM, respectively) and exhibits much reduced or little activity against more than 280 other kinases (IC50 >1μM). Reported to be orally available in dog, mouse, and rat with good pharmacokinetics and retard the growth of established PxBC-3 tumor mass in mice in vivo (by 20% and 59% at the end of a 21 day treatment period with b.i.d. oral dosage of 50 and 150mg/kg, respectively). The preincubation time-dependent inhibition, extremely slow dissociation rate, as well as the observed PERK selectivity, are all consistent with the inhibitor targeting PERK in its inactive DFG conformation.
TRUSTED_SUSTAINABILITY

Specifications

Formulation A 25 mM (2mg/177μL) sterile-filtered solution of PERK Inhibitor I, GSK2606414 in DMSO.
Description 98% by HPLC
Target Proteins PERK
Molecular Formula C24H20F3N5O
Formula Weight 451.4g/mol
Content And Storage Avoid Freeze-Thaw Cycles, Hygroscopic, Protect from Light
Form Liquid
Quantity 2 mg
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