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CHIR-98014

CAS No. : 252935-94-7

MCE 国际站：CHIR-98014

产品活性：CHIR-98014 是一种有效的，细胞通透的 GSK-3 抑制剂，可抑制 GSK-3α 和 GSK-3β 的活性，IC₅₀ 值分别为 0.65 和 0.58 nM；CHIR-98014 对 cdc2 和 erk2 的作用较弱。

研究领域：PI3K/Akt/mTOR  |  Stem Cell/Wnt

作用靶点：GSK-3

In Vitro: CHIR 98014 inhibits human GSK-3β with K_i value of 0.87 nM. CHIR 98014 causes GS stimulation in CHO-IR cells and rat hepatocytes, with EC₅₀s of 106 nM and 107 nM, respectively. CHIR-98014 (1 μM) reduces the viability of ES-CCE cells by 52%, with IC₅₀ of 1.1 μM. Moreover, CHIR-98014 in combination with CHIR-99021 results in a significant activation of the Wnt/beta-catenin pathway in ES-D3 cells. In CHIR-98014 treated cells, the T gene expression is induced up to 2,500-fold. CHIR-98014 (1 μM) also yields around 50% Brachyury-positive cells, with EC₅₀ of 0.32 μM. CHIR98014 (10 μM) prevents loss of neurites caused by 20 μM PrP1-30 in cortical and hippocampal neurons, and substantially decreases the amount of dead cells.

In Vivo: CHIR 98014 (30 mg/kg, i.p.) exhibits a significant reduction in fasting hyperglycemia within 4 h of treatment and shows improved glucose disposal during an ipGTT in markedly diabetic and insulin-resistant db/db mice.

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