GCN2iB 是一种 ATP 竞争性的一般控制非抑制性 2 抑制剂，IC50 为 2.4 nM。

GCN2iB is an ATP-competitive inhibitor of general control nonderepressible 2 (GCN2) with an IC50 of 2.4 nM.

GCN2iB shows an IC50 value of 2.4 nM for GCN2 and potent cellular activity.?In a panel of 468 kinases, only GCN2 shows >99.5% inhibition, and three kinases (MAP2K5, STK10, and ZAK) show >95%inhibition at 1 μM GCN2iB, demonstrating high kinase selectivity.

In the antitumor activity study of the CCRF-CEM xenografts, ASNase or GCN2iB alone does not significantly affect tumor growth.?Notably, a combination of ASNase and GCN2iB elicits potent antitumor activity (P=0.0002) with synergistic effects.?In MV-4-11 and SU.86.86 xenografts, the robust antitumor activity of the combination of GCN2iB and ASNase is observed with a synergistic effect, respectively.?ASNase/GCN2iB-treated tumors do not show significant growth even after drug cessation.

2183470-12-2

C18H12ClF2N5O3S

451.83

GCN2iB

DMSO:15 mg/mL (33.20 mM),Need ultrasonic
H2O:< 0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years