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GCN2iB

CAS No. : 2183470-12-2

MCE 国际站：GCN2iB

产品活性：GCN2iB 是具有 ATP 竞争性的、一种丝氨酸/苏氨酸蛋白激酶 压力应答激酶 (GCN2) 的抑制剂，其 IC₅₀ 值为 2.4 nM。

研究领域：Cell Cycle/DNA Damage | Autophagy

作用靶点：Eukaryotic Initiation Factor (eIF) | Autophagy

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 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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