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CHIR-99021 (CT99021)
产品纠错
CAS号:252917-06-9 | 英文名称:CHIR-99021 (CT99021)
分子式 C22H18Cl2N8
分子量 465
EINECS号 809-015-4
MDL MFCD11846251
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 CHIR-99021
英文名称 CHIR-99021
CAS号 252917-06-9
分子式 C22H18Cl2N8
分子量 465.34
EINECS号 809-015-4
物化性质
沸点 784.1±70.0 °C(Predicted)
密度 1.48
溶解度 DMSO:可溶,2mg/mL,澄清(加热)
形态 粉末
酸度系数(pKa) 11.92±0.10(Predicted)
颜色 白色至浅棕色
稳定性 DMSO中的溶液可在-20°下稳定储存3个月。
安全信息
危险品标志 T
危险类别码 25-36/37/38
安全说明 26-36/37/39-45
危险品运输编号 UN 2811 6.1 / PGIII
WGK Germany 3
海关编码 29335990
生产及用途
CHIR99021是一种氨基嘧啶衍生物,其抑制GSK3α和GSK3β的IC50值分别为10和6.7 nM。CHIR-99021 (CT99021)是一种GSK-3α和GSK-3β抑制剂, IC50分别为10 nM and 6.7 nM。CHIR99201对CDKs没有交叉反应性,对GSK-3β的选择性是对CDKs选择性的350倍。CHIR-99021 可作为Wnt/β-catenin的激活剂并诱导自噬。
TargetValue
GSK-3β
(Cell-free assay)
6.7 nM
GSK-3α
(Cell-free assay)
10 nM

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.

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产品供应商
252917-06-9
上海阿拉丁生化科技股份有限公司
2023-10-02

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