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化工儀器網>產品展廳>試劑標物>行業(yè)專用試劑>生物試劑>CT99021 CHIR-99021

CT99021 CHIR-99021

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  • 公司名稱 MedChemExpress LLC
  • 品牌 MedChemExpress (MCE)
  • 型號 CT99021
  • 產地
  • 廠商性質 生產廠家
  • 更新時間 2020/1/7 9:02:23
  • 訪問次數 797

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供貨周期 現貨 規(guī)格 10 mM * 1 mL;2 mg;5 mg
貨號 HY-10182 應用領域 生物產業(yè)

CHIR-99021

產品活性: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。

研究領域:PI3K/Akt/mTOR  |  Stem Cell/Wnt  |  Autophagy

作用靶點: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.

相關產品: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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