1782235-14-6
|
|
|
- CAS号:
- 1782235-14-6
- 英文名:
- CHIR 99021 trihydrochloride
- 英文别名:
- CHIR-99021 3HCl;CT-99021 trihydrochloride);CHIR 99021 trihydrochloride;Laduviglusib trihydrochloride;Laduviglusib (CHIR99021) trihydrochloride;CHIR 99021 trihydrochloride (252917-06-9 free base);CHIR-99021 trihydrochloride
(CT99021 trihydrochloride;CT99021 TRIHYDROCHLORIDE;CHIR99021 TRIHYDROCHLORIDE;CHIR 99021 TRIHYDROCHLORIDE;CT-99021 TRIHYDROCHLORIDE;6-((2-((4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)amino)nicotinonitrile trihydrochloride;6-[[2-[[4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile trihydrochloride
- 中文名:
- 1782235-14-6
- 中文别名:
- 化合物 T22657;GSK-3Α/Β抑制剂(CHIR-99021 TRIHYDROCHLORIDE);6-((2-((4-(2,4-二氯苯基)-5-(5-甲基-1H-咪唑-2-基)嘧啶-2-基)氨基)乙基)氨基)烟腈三盐酸盐
- CBNumber:
- CB63037186
- 分子式:
- C22H19Cl3N8
- 分子量:
- 501.8
- MOL File:
- 1782235-14-6.mol
|
|
|
1782235-14-6化学性质
-
储存条件:
-
Store at -20°C
-
|
-
溶解度:
-
DMSO:30.37(Max Conc. mg/mL);52.84(Max Conc. mM)
Water:16.69(Max Conc. mg/mL);29.04(Max Conc. mM)-
|
1782235-14-6性质、用途与生产工艺
CHIR-99021 trihydrochloride (CT99021 trihydrochloride) 是一种有效的选择性 GSK-3α/β 抑制剂，IC50 为 10 nM 和 6.7 nM。CHIR-99021 trihydrochloride 对 GSK-3 的选择性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。CHIR-99021 trihydrochloride 还是一种有效的 Wnt/β-catenin 信号通路激活剂。CHIR-99021 trihydrochloride 可增强小鼠和人类胚胎干细胞的自我更新。CHIR-99021 trihydrochloride 能诱导细胞自噬 (autophagy)。
|
GSK-3β
6.7 nM (IC
50
)
|
GSK-3α
10 nM (IC
50
)
|
cdc2
8800 nM (IC
50
)
|
CHIR-99021 inhibits human GSK-3β with K
i
values of 9.8 nM. CHIR-99021 is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that CHIR-99021 specifically inhibits GSK3β (IC
50
=~5 nM) and GSK3α (IC
50
=~10 nM), with little effect on other kinases. In the presence of CHIR-99021 the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM CHIR-99021 with an IC
50
of 4.9 μM.
In ZDF rats, a single oral dose of CHIR-99021 (16 mg/kg or 48 mg/kg) rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration. CHIR99021 (2 mg/kg) given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). CHIR99021 treatment significantly blocks crypt apoptosis and accumulation of p-H2AX
+
cells, and improves crypt regeneration and villus height. CHIR99021 treatment increases Lgr5
+
cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h.
1782235-14-6
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 |
|---|
| 2024/01/25 | HY-10182B | 1782235-14-6
Laduviglusib trihydrochloride | 1782235-14-6 | 2 mg | 650元 |
| 2024/01/25 | HY-10182B | 1782235-14-6
Laduviglusib trihydrochloride | 1782235-14-6 | 5 mg | 960元 |
1782235-14-6, 1782235-14-6 相关搜索:
- 细胞生物学试剂
- 化合物 T22657
- 6-((2-((4-(2,4-二氯苯基)-5-(5-甲基-1H-咪唑-2-基)嘧啶-2-基)氨基)乙基)氨基)烟腈三盐酸盐
- GSK-3Α/Β抑制剂(CHIR-99021 TRIHYDROCHLORIDE)
- 1782235-14-6
- Laduviglusib (CHIR99021) trihydrochloride
- Laduviglusib trihydrochloride
- CHIR 99021 trihydrochloride (252917-06-9 free base)
- 6-((2-((4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)amino)nicotinonitrile trihydrochloride
- CT-99021 trihydrochloride)
- CHIR-99021 trihydrochloride
(CT99021 trihydrochloride
- 6-[[2-[[4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile trihydrochloride
- CT99021 TRIHYDROCHLORIDE;CHIR99021 TRIHYDROCHLORIDE;CHIR 99021 TRIHYDROCHLORIDE;CT-99021 TRIHYDROCHLORIDE
- CHIR-99021 3HCl
- CHIR 99021 trihydrochloride