GCN2iB | GCN2 inhibitor | Probechem Biochemicals

Chemical Structure : GCN2iB

CAS No.: 2183470-12-2

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GCN2iB (GCN2 inhibitor)

货号: PC-20012Not For Human Use, Lab Use Only.

GCN2iB (GCN2 inhibitor) is a potent, selective and ATP-competitive GCN2 inhibitor with IC50 of 2.4 nM.

规格	价格	库存
5 mg	￥1580	In stock
10 mg	￥2480	In stock
25 mg	￥4280	In stock
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100 mg		Get quote

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生物&药学活性

GCN2iB (GCN2 inhibitor) is a potent, selective and ATP-competitive GCN2 inhibitor with IC50 of 2.4 nM.
GCN2iB displayed high selectivity against a panel of 468 kinases, only GCN2 showed >99.5% inhibition, and three kinases (MAP2K5, STK10, and ZAK) showed >95% inhibition at 1 uM.
GCN2iB exhibited in vitro antiproliferative effects in combination with ASNase against GCN2-WT MEF cells, but not against GCN2-KO MEF cells.
GCN2iB suppressed GCN2 pathway activation in xenograft models, a combination of L-asparaginase (ASNase) and GCN2iB elicited potent antitumor activity in CCRF-CEM xenografts and ALL xenograft model (MOLT-3) without severe body weight loss, but not ASNase or GCN2iB alone treatment.
The combination of ASNase treatment with GCN2 inhibition synergistically blocks in vivo tumor growth in ALL, AML, and pancreatic xenograft models.

物理化学性质&存储条件

分子量	451.83
分子式	C18H12ClF2N5O3S
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	N-(3-((2-aminopyrimidin-5-yl)ethynyl)-2,4-difluorophenyl)-5-chloro-2-methoxypyridine-3-sulfonamide

参考文献

1. Akito Nakamura, et al. Proc Natl Acad Sci U S A. 2018 Aug 14;115(33):E7776-E7785.

GCN2iB (GCN2 inhibitor)

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GCN2iB (GCN2 inhibitor)

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