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)。

Laduviglusib (CHIR-99021) trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC 50 s of 10 nM and 6.7 nM. Laduviglusib trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride induces autophagy.

Solid

GSK-3β 6.7 nM (IC50) GSK-3α 10 nM (IC

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.
[2]. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors.BMC Res Notes. 2014 Apr 29;7:273.

In Vitro: DMSO : ≥ 32 mg/mL (55.68 mM)H₂O : 19 mg/mL (33.06 mM; Need ultrasonic and warming)