| Bioactivity | GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM. | ||||||||||||
| Invitro | GSK2656157 results in inhibition of PERK activation as well as decreases in the downstream substrates, phospho-eIF2α, ATF4, and CHOP with an IC50 in the range of 10-30 nM in the BxPC3 pancreatic tumor cell line. Cells that are exposed to 1 μM GSK2656157 before UPR induction are able to block this effect on de novo protein synthesis[1]. GSK2656157 causes the activation of another eIF2α kinase to compensate for the loss of PERK activity in HT1080 cells. GSK2656157 inhibits the growth of the HT1080 cells[2]. GSK2656157 inhibits LPS-induced IL-1β production, LPS-induced Caspase 1 activation and LPS-induced eIF-2α phosphorylation, but does not inhibit LPS-induced TNF-α production[3]. | ||||||||||||
| Name | GSK2656157 | ||||||||||||
| CAS | 1337532-29-2 | ||||||||||||
| Formula | C23H21FN6O | ||||||||||||
| Molar Mass | 416.45 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
GSK2656157
CAS: 1337532-29-2 F: C23H21FN6O W: 416.45
GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PER
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.