GCN2 inhibitor 39

Chemical Structure : GCN2 inhibitor 39

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货号: PC-49370Not For Human Use, Lab Use Only.

GCN2 inhibitor 39 is a highly potent and selective, orally active inhibitor of general control nonderepressible 2 (GCN2) with IC50 of 5 nM.

规格	价格	库存	数量
10 mg		Get quote
25 mg		Get quote
50 mg		Get quote

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生物&药学活性

GCN2 inhibitor 39 is a highly potent and selective, orally active inhibitor of general control nonderepressible 2 (GCN2) with IC50 of 5 nM.
GCN2 inhibitor 39 displays excellent selectivity against its closely related Integrated Stress Response (ISR) family members heme-regulated inhibitor kinase (HRI), PKR, and (PKR)-like endoplasmic reticulum kinase (PERK).
GCN2 inhibitor 39 engages GCN2 at levels ≥80% with an oral dose of 15 mg/kg BID in mice.
GCN2 inhibitor 39 alleviates MDSC-related T cell suppression and restore T cell proliferation, similar to the effect seen in MDSCs from GCN2 knockout mice.
GCN2 inhibitor 39 (50 mg/kg, BID) demonstrates significant tumor growth inhibition (TGI) as a single agent in the LL2 syngeneic mouse model, also enhances TGI mediated by anti-VEGFR.

物理化学性质&存储条件

分子量	527.445
分子式	C22H23BrN8OS
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(1R,3R)-3-((3-bromo-1-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl)amino)-N,1-dimethylcyclopentane-1-carboxamide

参考文献

1. Jeffrey J. Jackson, et al. Journal of Medicinal Chemistry, 2022