CHIR99021

CHIR99021 is a potent and selective GSK-3 inhibitor that has been widely used in research. It is a small molecule that has been shown to have a variety of effects on cells, including promoting self-renewal and pluripotency in embryonic stem cells, and inducing Wnt signaling pathway, which is involved in many aspects of development and disease.

Chemistry

CHIR99021 is a synthetic molecule that belongs to the class of pyrimidine derivatives. It is a potent and selective inhibitor of glycogen synthase kinase 3 (GSK-3), with IC50 values of 7 nM for GSK-3β and 10 nM for GSK-3α. The selectivity of CHIR99021 for GSK-3 is greater than 500-fold compared to other kinases.

Mechanism of Action

CHIR99021 acts by inhibiting the activity of GSK-3, a kinase that is involved in a variety of cellular processes, including cell proliferation, cell differentiation, and cell death. By inhibiting GSK-3, CHIR99021 can promote the self-renewal and pluripotency of embryonic stem cells, and induce the Wnt signaling pathway.

Applications in Research

CHIR99021 has been widely used in research due to its potent and selective inhibition of GSK-3. It has been used to maintain the pluripotency of embryonic stem cells in culture, and to induce the Wnt signaling pathway in various cell types. In addition, CHIR99021 has been used in studies investigating the role of GSK-3 in disease, including cancer, neurodegenerative diseases, and diabetes.

Safety and Toxicity

As a research chemical, CHIR99021 is not intended for use in humans. However, studies in animals have shown that it can cause side effects, including weight loss and changes in blood chemistry. The safety and toxicity of CHIR99021 in humans is not known.

See Also

• Glycogen synthase kinase 3
• Wnt signaling pathway
• Embryonic stem cells