化合物Laduviglusib三盐酸盐 T22657

Product Introduction
Bioactivity


英文名: Laduviglusib trihydrochloride

描述: Laduviglusib trihydrochloride (CT99021 trihydrochloride) 是一种选择性糖原合成酶激酶 3 (GSK-3) 抑制剂，对 GSK-3α 和 GSK-3β 的 IC50 分别为 10 nM 和 6.7 nM。 Laduviglusib trihydrochloride 抑制人 GSK-3β，Ki 为 9.8 nM。 Laduviglusib trihydrochloride 是 Wnt/β-catenin 信号通路的激活剂。 Laduviglusib trihydrochloride 诱导自噬。

体外活性: Laduviglusib trihydrochloride(10 μM) lowers the viability of the ES-D3 cells by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% with an IC50 of 4.9 μM[2]. Laduviglusib trihydrochloride shows >500-fold selectivity over ERK2, CDC2, and other protein kinases. Laduviglusib trihydrochloride specifically inhibits GSK3β and GSK3α with IC50s of 5nM and 10nM in vitro kinase assays[4].

体内活性: Oral administration of Laduviglusib trihydrochloride(16 mg/kg and 48 mg/kg) rapidly reduces plasma glucose with a maximal reduction of nearly 150 mg/dl in ZDF rats[1]. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride (2 mg/kg) improves survival after 14.5 Gy abdominal irradiation. Laduviglusib trihydrochloride inhibits crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. Laduviglusib trihydrochloride blocks apoptosis, increases Lgr5+ cell survival and prevents the reduction of Olfm4, Lgr5 and CD44[5].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 17.1 mg/mL (29.8 mM)
DMSO : 28.8 mg/mL (50.1 mM)


关键字: 252917-06-9 free base | CHIR 99021 Trihydrochloride | Laduviglusib | CHIR99021 Trihydrochloride | CT99021 Trihydrochloride | CT-99021 Trihydrochloride | CT 99021 Trihydrochloride | CT99021 | CHIR 99021 | 252917-06-9 | CHIR99021 | CHIR-99021 | CHIR-99021 Trihydrochloride | CT-99021 | Laduviglusib Trihydrochloride | CT 99021

相关产品: Cromolyn sodium | 4,10-Aromadendranediol | 1-Azakenpaullone | LY2090314 | MBM-55S | Indirubin-3′-oxime | (E/Z)-GSK-3β inhibitor 1 | Cyanoacetohydrazide | Indirubin | Isoangustone A

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | Anti-Obesity Compound Library | Metabolism Compound Library | Bioactive Compound Library

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