1025015-40-0
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- CAS号:
- 1025015-40-0
- 英文名:
- GK921
- 英文别名:
- 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]-
- 中文名:
- 1025015-40-0
- 中文别名:
- 化合物GK921;转谷氨酰胺酶2(TGASE2)抑制剂(GK921);3-(苯基乙炔基)-2-(2-(吡咯烷-1-基)乙氧基)吡啶并[2,3-B]吡嗪
- CBNumber:
- CB42715630
- 分子式:
- C21H20N4O
- 分子量:
- 344.41
- MOL File:
- 1025015-40-0.mol
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1025015-40-0化学性质
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储存条件:
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Store at -20°C
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溶解度:
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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)-
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形态:
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A solid
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1025015-40-0性质、用途与生产工艺
GK921是transglutaminase 2 (TGase 2)抑制剂，IC50为8.93 μM。
| Target | Value |
TGase 2
()
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8.93 μM
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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.
A single treatment with GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models.
1025015-40-0
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
1025015-40-0, 1025015-40-0 相关搜索:
- 药靶配体
- 细胞生物学试剂
- 3-(苯基乙炔基)-2-(2-(吡咯烷-1-基)乙氧基)吡啶并[2,3-B]吡嗪
- 化合物GK921
- 转谷氨酰胺酶2(TGASE2)抑制剂(GK921)
- 1025015-40-0
- 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]-
- GK921, >98%
- GK-921;GK 921
- 3-(phenylethynyl)-2-(2-(pyrrolidin-1-yl)ethoxy)pyrido[3,2-b]pyrazine
- GK921