CT99021 CHIR-99021
- 公司名稱 MedChemExpress LLC
- 品牌 MedChemExpress (MCE)
- 型號(hào) CT99021
- 產(chǎn)地
- 廠商性質(zhì) 生產(chǎn)廠家
- 更新時(shí)間 2020/1/7 9:02:23
- 訪問(wèn)次數(shù) 864
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抑制劑，調(diào)節(jié)劑，API，天然產(chǎn)物，各種類型化合物庫(kù)
| 供貨周期 | 現(xiàn)貨 | 規(guī)格 | 10 mM * 1 mL；2 mg；5 mg |
|---|---|---|---|
| 貨號(hào) | HY-10182 | 應(yīng)用領(lǐng)域 | 生物產(chǎn)業(yè) |
CHIR-99021
產(chǎn)品活性：CHIR-99021是 GSK-3α/β 抑制劑， IC50 分別為 10 nM，6.7 nM。 抑制 GSK-3α/β 比同源物 CDC2 和 ERK2 高 500 倍。
研究領(lǐng)域：PI3K/Akt/mTOR | Stem Cell/Wnt | Autophagy
作用靶點(diǎn)：GSK-3 | Autophagy
In Vitro: 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: 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.
相關(guān)產(chǎn)品：Kinase Inhibitor Library | Stem Cell Signaling Compound Library | PI3K/Akt/mTOR Compound Library | Anti-Cancer Compound Library | Bioactive Compound Library Plus | Autophagy Compound Library | Wnt/Hedgehog/Notch Compound Library | SB 216763 | TWS119 | LY2090314 | GSK 3 Inhibitor IX | Tideglusib | Kenpaullone | AR-A014418 | CHIR-99021 trihydrochloride | AZD2858 | AZD1080 | Indirubin-3'-monoxime | RGB-286638 free base | SB 415286 | Bikinin | TDZD-8 | CHIR-98014 | IM-12 | CP21R7 | BIO-acetoxime | EHT 5372 | GSK-3 inhibitor 1 | 5-Iodo-indirubin-3'-monoxime | GSK-3β inhibitor 1 | Indirubin-3'-monoxime-5-sulphonic acid | Indirubin-5-sulfonate
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