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 |
|
others | Enquire |
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 |