GK921|1025015-40-0|-陌孚医药/Medlife

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GK921

目录号: PL02602 纯度: ≥99%

CAS No. :1025015-40-0

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产品详情	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。
生物活性	GK921 is a transglutaminase 2 (TGase) inhibitor with an IC 50 of 7.71 μM for human recombinant TGase 2.
性状	Solid
IC50 & Target[1][2]	IC50: 7.71 μM (TGase)
体外研究(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 to 10 M. The average GI50 is 9.05×10 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Ku BM, et al. Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft models. J Cancer Res Clin Oncol. 2014 May;140(5):757-67.

溶解度数据	In Vitro: DMSO : ≥ 30 mg/mL (87.11 mM)配制储备液

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