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抑制剂描述:

产品名称:GK921

产品别名:见爱必信官网

英文别名:GK921

靶点:Tgase

CAS:1025015-40-0

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

GK921 is a transglutaminase 2 (TGase 2) inhibitor with average GI50 of 0.9 uM in cancer cell lines.

溶解性:DMSO : ≥ 30 mg/mL (87.11 mM)

体外研究:

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.

体内研究: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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