1025015-40-0
中文名稱
1025015-40-0
英文名稱
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
2024/12/23 09:08:08
1025015-40-0 結(jié)構(gòu)式
基本信息
中文別名
化合物GK921轉(zhuǎn)谷氨酰胺酶2(TGASE2)抑制劑(GK921)
英文別名
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]-
所屬類別
生物化工：激動(dòng)劑抑制劑物理化學(xué)性質(zhì)
儲(chǔ)存條件-20°C儲(chǔ)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)
形態(tài)固體
顏色Off-white to brown
常見(jiàn)問(wèn)題列表
生物活性
GK921是transglutaminase 2 (TGase 2)抑制劑，IC50為8.93 μM。靶點(diǎn)
| Target | Value |
|
TGase 2
() | 8.93 μM |
體外研究
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.
體內(nèi)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.