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 2026/07/13 11:29:12

1025015-40-0 結(jié)構(gòu)式

基本信息物理化學(xué)性質(zhì) 安全數(shù)據(jù) 圖譜信息 1025015-40-0價(jià)格(試劑級(jí)) 常見問題列表

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

GK921
GK921, >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)

形態(tài)固體

顏色Off-white to brown

InChI1S/C21H20N4O/c1-2-7-17(8-3-1)10-11-19-21(26-16-15-25-13-4-5-14-25)24-18-9-6-12-22-20(18)23-19/h1-3,6-9,12H,4-5,13-16H2

InChIKeyMNYJJHBAEYKXEG-UHFFFAOYSA-N

SMILESN4(CCCC4)CCOc1nc2c(nc1C#Cc3ccccc3)nccc2

安全數(shù)據(jù)

WGK GermanyWGK 3

存儲(chǔ)類別11 - Combustible Solids

圖譜信息

1025015-40-0(1025015-40-0)核磁圖(¹HNMR)

1025015-40-0價(jià)格(試劑級(jí))

報(bào)價(jià)日期	產(chǎn)品編號(hào)	產(chǎn)品名稱	CAS號(hào)	包裝	價(jià)格
2026/07/06	S6417	1025015-40-0 GK921	1025015-40-0	2mg	1204.39元
2026/07/06	S6417	1025015-40-0 GK921	1025015-40-0	5mg	2375.4元
2026/06/05	HY-12337	1025015-40-0 GK921	1025015-40-0	1 mg	706元

常見問題列表

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.