LaduviglusibLaduviglusib
MedChemExpress (MCE)
HY-10182
252917-06-9
CHIR-99021
CT99021
99.43%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Room temperature in continental US
may vary elsewhere.
Laduviglusib (CHIR-99021) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy.
Laduviglusib (1-10 μM, 3 days) reduces the viability of the ES-D3 cells with an IC50 of 4.9 μM[2]. Laduviglusib (5 μM, 48 h) activates the canonical Wnt-pathway in ES-D3 cells and ES-CCE cells[2]. Laduviglusib (3 μM, 4 days) inhibits ES cell differentiation into neural cells[3]. Laduviglusib (1 μM, 2 weeks) inhibits adipogenesis by blocking induction of C/EBPα and PPARγ in 3T3-L1 preadipocytes[4]. Laduviglusib (2.5 μM, 24 h) protects Lgr5+ cells against radiation-induced apoptosis[5].
Laduviglusib (30 mg/kg, p.o) rapidly lowers plasma glucose[1]. Laduviglusib (2 mg/kg, i.p.) protects mice against radiation-induced lethal GI injury[5].
GSK-3β 6.7 nM (IC50) GSK-3α 10 nM (IC50) cdc2 8800 nM (IC50)
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[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar
52(3):588-95. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[4]. Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23
277(34):30998-1004. [Content Brief]
[5]. Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10
5:8566. [Content Brief]