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簡要描述：CHIR-99021 252917-06-9CHIR-99021 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.
產(chǎn)品型號(hào)：abs810052廠商性質(zhì)：生產(chǎn)廠家更新時(shí)間：2026-02-24訪 問 量：2092產(chǎn)品分類
Product Category詳細(xì)介紹
| 品牌 | absin | CAS | 252917-06-9 |
|---|---|---|---|
| 分子式 | C22H18Cl2N8 | 純度 | ＞98% |
| 分子量 | 465.34 | 貨號(hào) | abs810052 |
| 規(guī)格 | 5mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a GSK-3α/β inhibitor with IC50 of 10 | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
CHIR-99021 252917-06-9
| 產(chǎn)品描述 | |
| 描述 | CHIR-99021 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. |
| 純度 | ＞98% |
| 活性 | IC50: 10 nM/6.7 nM (GSK-3α/β) |
| 儲(chǔ)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 | |
| 別名 | Laduviglusib；CT99021; CHIR99021; CHIR 99021; CT-99021 |
| 外觀 | white to light brown powder |
| 可溶性/溶解性 | DMSO：10 mg/mL warmed (21.48 mM) |
| 生物活性 | |
| 靶點(diǎn) | GSK-3β,GSK-3α |
| In vitro(體外研究) | 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(體內(nèi)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. |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | Cell CycleKinases/PhosphatasesCdksEpigeneticsCell cycleKinases/PhosphatasesCdksNeuroscienceNeurology processNeural Signal TransductionNeuroscienceNeurology processNeurodegenerative diseaseOtherDrug DiscoverySmall Molecule DrugLead Compound Discovery |
CHIR-99021 252917-06-9 溫馨提示：本產(chǎn)品僅作科研實(shí)驗(yàn)使用，不支持臨床等研究
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