| Bioactivity | 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[1][2][3]. | ||||||||||||
| Invitro | 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]. Cell Viability Assay[2] Cell Line: | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | Laduviglusib | ||||||||||||
| CAS | 252917-06-9 | ||||||||||||
| Formula | C22H18Cl2N8 | ||||||||||||
| Molar Mass | 465.34 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [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]. Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004. [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. |
Laduviglusib
CAS: 252917-06-9 F: C22H18Cl2N8 W: 465.34
Laduviglusib (CHIR-99021) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM.
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