GK921 |CAS:1025015-40-0 Probechem Biochemicals

Chemical Structure : GK921

CAS No.: 1025015-40-0

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GK921 (GK 921;GK-921)

货号: PC-42986Not For Human Use, Lab Use Only.

GK921 is a specific, orally active Transglutaminase 2 (TGase 2, TG2) inhibitor with IC50 of 7.71 uM against recombinant hTGase 2.

规格	价格	库存
5 mg	￥1880	In stock
25 mg	￥3680	In stock
100 mg	￥9880	In stock
500 mg		Get quote
1 g		Get quote

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生物&药学活性

GK921 is a specific, orally active Transglutaminase 2 (TGase 2, TG2) inhibitor with IC50 of 7.71 uM against recombinant hTGase 2.
GK921 inhibits the TGase 2-induced polymerization of I-κBα and p53 in vitro in a dose-dependent manner, induces cell death of eight RCC lines with average GI50 of 0.9 uM.
GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models.
GK921 blocks MES transdifferentiation and showed significant therapeutic efficacy in mouse models of glioma stem cells (GSC)

物理化学性质&存储条件

分子量	344.4097
分子式	C21H20N4O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	DMSO: ≥ 30 mg/mL
Chemical Name/SMILES	Pyrido[2,3-b]pyrazine, 3-(2-phenylethynyl)-2-[2-(1-pyrrolidinyl)ethoxy]-

参考文献

1. Yin J, et al. Cancer Res. 2017 Sep 15;77(18):4973-4984.

2. Kang JH, et al. Cell Death Dis. 2016 Apr 21;7:e2200.

3. Ku BM, et al. J Cancer Res Clin Oncol. 2014 May;140(5):757-67.

4. Kang JH, et al. Cell Death Dis. 2016 Mar 31;7:e2163.

GK921 (GK 921;GK-921)

生物&药学活性

物理化学性质&存储条件

参考文献

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GK921 (GK 921;GK-921)

生物&药学活性

物理化学性质&存储条件

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