2109414-84-6
Chemical Structure
Laduviglusib dihydrochloride
Synonym(s): CHIR-99021 dihydrochloride; CT99021 dihydrochloride
- CAS No.: 2109414-84-6
- Formula:C22H20Cl4N8
- Molecular Weight:538.26
IUPAC Name: 6-((2-((4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)amino)nicotinonitrile dihydrochloride
InChIKey: OOMHEMQQCHEWDS-UHFFFAOYSA-N
SMILES: N#CC1=CC=C(N=C1)NCCNC2=NC=C(C(C3=CC=C(Cl)C=C3Cl)=N2)C4=NC=C(N4)C.[H]Cl.[H]Cl
Biological Activity: Laduviglusib dihydrochloride (CHIR-99021 dihydrochloride; CT99021 dihydrochloride) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib dihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib dihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib dihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib dihydrochloride induces autophagy[1][2][3].
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Laduviglusib dihydrochloride | Laduviglusib dihydrochloride (CHIR-99021 dihydrochloride; CT99021 dihydrochloride) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib dihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib dihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib dihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib dihydrochloride induces autophagy. | |||||||||||||||||||||
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References
- [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]
