Description
CHIR-99021 (CT99021) is an inhibitor of GSK-3α/β with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.
Product Overview
CHIR-99021 is a highly specific glycogen synthase kinase-3 (GSK-3) inhibitor which can inhibit both isoforms with IC50 of 10 nM (GSK-3α) and 6.7 nM (GSK-3β). CHIR-99021 was proved to promote self-renewal and maintain pluripotency of both B6 and BALB/c ES cells via stabilizing the downstream effectors like c-Myc and β-catenin. In J1 mESC cells, CHIR-99021 played an important role in maintaining the colony morphology as well as the self-renewal when combined with leukemia inhibitory factor (LIF). CHIR-99021 has shown to regulate multiple signaling pathways which involve Wnt/β-catenin, TGF-β, Nodal and MAPK, and the expression of epigenetic regulatory genes like Dnmt3l. CHIR-99021 has been demonstrated to promote DN3 thymocytes proliferation and differentiation in the absence of pre-TCR signaling, Notch1 signaling or CXCL12.However, study has also found that higher concentration (10 nM but not 1 nM or 3 nM) of CHIR99021 might selectively inhibit differentiation by activating IL-7 signaling pathway.
Synonyms
CHIR99021, CHIR-99021, CHIR 99021, CT99021,GSK-3 Inhibitor XVI
Molecular Formula
C22H18Cl2N8
Chemical Name
6-[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl]amino]ethylamino]pyridine-3-carbonitrile
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request