GCN2iB

Research use only, not for human use.

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

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

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 elicit potent antitumor activity (P=0.0002) with synergistic effects. In MV-4-11 and SU.86.86 xenografts, robust antitumor activity of the combination of GCN2iB and ASNase is observed with synergistic effect, respectively. ASNase/GCN2iB-treated tumors do not show significant growth even after drug cessation. The combination of ASNase and GCN2iB yield survival advantage compared with the vehicle treated control with synergistic effect.

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Others

Other Targets

Antibacterial

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2183470-12-2

451.83

C18H12ClF2N5O3S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (110.66 mM)

COc1ncc(Cl)cc1S(=O)(=O)Nc1ccc(F)c(C#Cc2cnc(N)nc2)c1F

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(-20℃)

With Ice Pack

≥ 2 years