CHIR99021

CHIR99021 is an aminopyrimidine derivative. CHIR99021 promotes self-renewal potential of embryonic stem cells (ESCs) of mice by inhibiting glycogen synthase kinase-3 (GSK-3) activity and potentiates the upregulation of β-catenin and c-Myc functions. CHIR99021 promotes self-renewal of ESCs by modulating transforming growth factor β (TGF-β), Notch and mitogen-activated protein kinases (MAPK) signaling pathways. CHIR99021 is an agonist of wingless/integrated (wnt) signalling, upregulates cyclinA expression and promotes cell proliferation in non-small-cell lung cancer (NSCLC) cell lines.

CHIR99021 has been used as a Wnt signaling agonist to study its effects on the differentiation of human pluripotent stem cell-derived cardiomyocytes (hPSCs).

CHIR99021 has been used:

• in cocktail with small molecules to convert human lung fibroblast cells into neurons
• as a culture medium supplement in potassium supplemented simplex optimization medium (KSOM) for the culture of blastocysts
• for chronic inhibition of GSK-3 to investigate its role in corticogenesis

CHIR99021 is a very potent inhibitor of Glycogen synthase kinase 3 (GSK3, IC₅₀ values for GSK3α and GSK3β = 10 and 6.7 nM, respectively). There is no cross-reactivity against CDKs. CHIR99201 potentiates self-renewal of human and mouse embryonic stem cells, and enhances reprogramming of somatic cells into stem cells.

CHIR99021 is a very potent inhibitor of Glycogen synthase kinase 3.