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CHIR-99021 trihydrochloride
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CHIR-99021 trihydrochloride
CAS No. : 1782235-14-6
MCE 站:CHIR-99021 trihydrochloride
产品活性:CHIR-99021 trihydrochloride (CT99021 trihydrochloride) 是一种有效的选择性 GSK-3α/β 抑制剂,IC50 为 10 nM 和 6.7 nM。CHIR-99021 trihydrochloride 对 GSK-3 的选择性比 CDC2,ERK2 和其他蛋白激酶高 500 倍以上。CHIR-99021 trihydrochloride 还是一种有效的 Wnt/β-catenin 信号通路激活剂。CHIR-99021 trihydrochloride 可增强小鼠和人类胚胎干细胞的自我更新。CHIR-99021 trihydrochloride 能诱导细胞自噬 (autophagy)。
研究领域:PI3K/Akt/mTOR | Stem Cell/Wnt | Autophagy
作用靶点:GSK-3 | Wnt | β-catenin | Autophagy
In Vitro: CHIR-99021 inhibits 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.
相关产品:Bioactive Compound Library Plus | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Wnt/Hedgehog/Notch Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Neuroprotective Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | CHIR-99021 | XAV-939 | IWR-1 | SB 216763 | IWP-2 | Pyrvinium pamoate | Salinomycin | Heparan Sulfate | BML-284 | AR-A014418 | TDZD-8 | Kenpaullone | GSK 3 Inhibitor IX | HLY78 | Cromolyn sodium | FH535 | Wogonin | Toxoflavin | Echinacoside | PNU-74654 | WAY-262611 | R547 | Tegatrabetan | SB 415286 | IM-12 | Indirubin-3'-monoxime | Prinaberel | 1-Azakenpaullone
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