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CAS No. : 1782235-14-6
MCE 国际站:Laduviglusib trihydrochloride
产品活性:Laduviglusib (CHIR-99021) 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。Laduviglusib trihydrochloride 还是一种有效的 Wnt/β-catenin 信号通路激活剂。Laduviglusib trihydrochloride 可增强小鼠和人类胚胎干细胞的自我更新。Laduviglusib 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: Laduviglusib trihydrochloride inhibits human GSK-3β with Ki values of 9.8 nM. Laduviglusib trihydrochloride is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that Laduviglusib trihydrochloride specifically inhibits GSK3β (IC50=~5 nM) and GSK3α (IC50=~10 nM), with little effect on other kinases. In the presence of Laduviglusib trihydrochloride 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 Laduviglusib trihydrochloride with an IC50 of 4.9 μM.
In Vivo: In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) trihydrochloride rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration. Laduviglusib (2 mg/kg) trihydrochloride given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib trihydrochloride treatment significantly blocks crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. Laduviglusib trihydrochloride treatment increases Lgr5+ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h.
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货号: HY-10182B
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