GSK2656157
- Catalog NO.:A888034
- CAS No. : 1337532-29-2
- Molecular Formula:C23H21FN6O
- Molecular Weight: 416.45
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Bulk Inquiry
1. Please click the to confirm the discount and stock quantity.
2. Click“Bulk Inquiry”to ask for quotations of other quantity.
3. The price does not include shipping and bank charges.
Quality Control&SDS
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. |