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| 品牌 | absin | CAS | 1782235-14-6 |
|---|---|---|---|
| 分子式 | C22H18Cl2N8.3HCl | 纯度 | ＞98% |
| 分子量 | 574.72 | 货号 | abs818359 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a GSK-3α/β inhibitor with IC50 of 10 | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
CHIR-99021 trihydrochloride 1782235-14-6
| 产品描述 | |
| 描述 | CHIR-99021 trihydrochloride is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. |
| 纯度 | ＞98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | Laduviglusib trihydrochloride；CT99021 trihydrochloride |
| 可溶性/溶解性 | DMSO: ≥ 32 mg/mL |
| 生物活性 | |
| 靶点 | GSK-3 |
| In vitro(体外研究) | CHIR 99021inhibits human GSK-3β with Ki 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 (IC50=~5 nM) and GSK3α (IC50=~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 IC50 of 4.9 μM. |
| In vivo(体内研究) | 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. |
| 研究领域 | |
| 研究领域 | Cell CycleKinases/PhosphatasesCdks EpigeneticsCell cycleKinases/PhosphatasesCdks NeuroscienceNeurology processNeural Signal Transduction NeuroscienceNeurology processNeurodegenerative diseaseOther Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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