For R&D use only.

GSK2656157

  • Catalog NO.:A888034
  • CAS No. : 1337532-29-2
  • Molecular Formula:C23H21FN6O
  • Molecular Weight: 416.45
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Product Details

CAS Number 1337532-29-2 Appearance
Catalog Number A888034 MDL Number MFCD27997885
Molecular Formula C23H21FN6O Molecular Weight 416.45
Boiling Point 744.6±60.0°C at 760 mmHg Melting Point
Flash Point Density
Synonyms 1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethanone
Storage Condition Store in a tightly closed container,in a cool and dry place

Safety

GHS Pictogram
Signal Word Warning UN Number
Hazard Statements H302 Class
Precautionary Statements P280-P305+P351+P338 Packing Group

Description

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.

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GSK2656157
1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethanone