产品说明书

Laduviglusib 3HCl

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Chemical Structure| 1782235-14-6 同义名 : CT99021 trihydrochloride;CHIR-99021 trihydrochloride;Laduviglusib trihydrochloride
CAS号 : 1782235-14-6
货号 : A962469
分子式 : C22H21Cl5N8
纯度 : 99%+
分子量 : 574.721
MDL号 : MFCD29079432
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(52.2 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 18 mg/mL(31.32 mM)
动物实验配方：
生物活性
描述 Laduviglusib 3HCl is an effective and selective inhibitor of GSK-3α/β, with IC50 values of 10 nM and 6.7 nM, respectively, acting through competitive binding at the ATP site to inhibit GSK3α and GSK3β. It is over 500 times more selective for GSK-3 than for CDC2, ERK2, and other protein kinases. Laduviglusib 3HCl is also an effective activator of the Wnt/β-catenin signaling pathway. It enhances self-renewal in both mouse and human embryonic stem cells and induces autophagy[1][2][3]. At a concentration of 2.5 μM, Laduviglusib 3HCl treatment reduces the viability of ES-D3 cells by 24.7%, at 5 μM by 56.3%, at 7.5 μM by 61.9%, and at 10 μM by 69.2%, with an IC50 of 4.9 μM[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.74mL

0.35mL

0.17mL

8.70mL

1.74mL

0.87mL

17.40mL

3.48mL

1.74mL
参考文献

[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.

[3]Ye S, et al. Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embryonic stem cells from refractory mouse strains. PLoS One. 2012;7(4):e35892.

[4]Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566.