1025015-40-0
中文名称
1025015-40-0
英文名称
GK921
CAS
1025015-40-0
分子式
C21H20N4O
分子量
344.41
MOL 文件
1025015-40-0.mol
更新日期
2024/05/27 17:16:38
1025015-40-0 结构式
基本信息
中文别名
化合物GK921转谷氨酰胺酶2(TGASE2)抑制剂(GK921)
英文别名
GK921GK921, >98%
GK-921
GK 921
3-(phenylethynyl)-2-(2-(pyrrolidin-1-yl)ethoxy)pyrido[3,2-b]pyrazine
3-(2-Phenylethynyl)-2-[2-(1-pyrrolidinyl)ethoxy]pyrido[2,3-b]pyrazine
Pyrido[2,3-b]pyrazine, 3-(2-phenylethynyl)-2-[2-(1-pyrrolidinyl)ethoxy]-
所属类别
生物化工：激动剂抑制剂物理化学性质
储存条件-20°C储存
溶解度DMF:30.0(Max Conc. mg/mL);87.1(Max Conc. mM)
DMSO:31.5(Max Conc. mg/mL);91.46(Max Conc. mM)
Ethanol:30.0(Max Conc. mg/mL);87.1(Max Conc. mM)
Ethanol:PBS (pH 7.2) (1:6):0.14(Max Conc. mg/mL);0.41(Max Conc. mM)
DMSO:31.5(Max Conc. mg/mL);91.46(Max Conc. mM)
Ethanol:30.0(Max Conc. mg/mL);87.1(Max Conc. mM)
Ethanol:PBS (pH 7.2) (1:6):0.14(Max Conc. mg/mL);0.41(Max Conc. mM)
形态固体
1025015-40-0价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/04/30 | HY-12337 | 1025015-40-0 GK921 | 1025015-40-0 | 2mg | 1000元 |
| 2024/04/30 | S6417 | 1025015-40-0 GK921 | 1025015-40-0 | 2mg | 1204.39元 |
| 2024/04/30 | HY-12337 | 1025015-40-0 GK921 | 1025015-40-0 | 10mM * 1mLin DMSO | 1894元 |
常见问题列表
生物活性
GK921是transglutaminase 2 (TGase 2)抑制剂，IC50为8.93 μM。靶点
| Target | Value |
|
TGase 2
() | 8.93 μM |
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 GI 50 of 10 -10 to 10 -4 M. The average GI 50 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.