GSK2656157

GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC50 of 0.9 nM. It is highly selective for PERK with IC50 values >100 nM against a panel of 300 kinases. GSK2656157 inhibits PERK activity in cells with an IC50 in the range of 10-30 nM as shown by inhibition of stress-induced PERK autophosphorylation, eIF2α substrate phosphorylation, together with corresponding decreases in ATF4 and CHOP proteins in multiple cell lines. Oral administration of GSK2656157 to mice shows a dose- and time-dependent pharmacodynamic response in pancreas as measured by PERK auto-phosphorylation.

Product information

CAS Number: 1337532-29-2

Molecular Weight: 416.45

Formula: C23H21FN6O

Chemical Name: 1-(5-{4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl}-4-fluoro-2,3-dihydro-1H-indol-1-yl)-2-(6-methylpyridin-2-yl)ethan-1-one

Smiles: CN1C=C(C2=C1N=CN=C2N)C1=CC=C2C(CCN2C(=O)CC2=CC=CC(C)=N2)=C1F

InChiKey: PRWSIEBRGXYXAJ-UHFFFAOYSA-N

InChi: InChI=1S/C23H21FN6O/c1-13-4-3-5-14(28-13)10-19(31)30-9-8-16-18(30)7-6-15(21(16)24)17-11-29(2)23-20(17)22(25)26-12-27-23/h3-7,11-12H,8-10H2,1-2H3,(H2,25,26,27)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.