GK921,1025015-40-0

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GK921

CAS No. : 1025015-40-0

MCE 国际站：GK921

产品活性：GK921是转谷氨酰胺酶2 (TGase2) 抑制剂，对人类重组TGase2的IC₅₀值为7.71 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Glutaminase

In Vitro: GK921 inhibits the TGase 2-induced polymerization of I-κBα and p53 in a dose-dependent manner. The cytotoxicity of GK921 ranged from GI₅₀ of 10^-10 to 10^-4 M. The average GI₅₀ is 9.05×10^-7 M. GK921 rescues p53 levels and consequently induces apoptosis; a concentration-dependent increase in cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels is observed.

In Vivo: A single treatment with GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models.

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