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CHIR-99021 monohydrochloride

CAS No. : 1797989-42-4

MCE 站：CHIR-99021 monohydrochloride

产品活性：CHIR-99021 monohydrochloride (CT99021 monohydrochloride) 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 monohydrochloride 对 GSK-3 的选择性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。CHIR-99021 monohydrochloride 还是一种有效的 Wnt/β-catenin 信号通路激活剂。CHIR-99021 monohydrochloride 可增强小鼠和人类胚胎干细胞的自我更新。CHIR-99021 monohydrochloride 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 K_i 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  |  Diabetes Related 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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