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A7754858

GSK2656157 , 10mMinDMSO , 1337532-29-2

CAS NO.:1337532-29-2

Empirical Formula: C23H21FN6O

Molecular Weight: 416.45

MDL number: MFCD27997885

Pack Size Price Stock Quantity
1ml RMB559.20 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Melting point: 194-196°C
Boiling point: 744.6±60.0 °C(Predicted)
Density  1.43±0.1 g/cm3(Predicted)
storage temp.  -20°C
solubility  Soluble in DMSO (10 mg/ml with warming)
form  solid
pka 5.32±0.30(Predicted)
color  White
Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

Description and Uses

GSK2656157 (1337532-29-2) is a potent (IC50 = 0.9 nM) and selective (over 300 kinases) inhibitor of protein kinase RNA-like endoplasmic reticulum kinase (PERK).1,2? Inhibited growth of multiple human tumor xenografts in mice. GSK2656157 has also been found to potently inhibit RIPK1 (IC50 = 69 nM) and TNF-mediated RIPK1 kinase-dependent cell death in mouse embryonic fibroblasts.3 It prevented the loss of dendritic spines and rescued memory deficits after traumatic brain injury.4? GSK2656157 also enhanced glucose-stimulated insulin secretion in a mouse model of type 2 diabetes mellitus.5

GSK2656157 is an ATP-competitive and highly selective inhibitor of PKR-like endoplasmic reticulum kinase (PERK) enzyme activity. GSK2656157 also has anti-tumor and anti-angiogenic activity.

Safety

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P264-P270-P301+P312-P330-P501

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