A-285222

A-285222 (also known as BTP-19) is a cell-permeable, low molecular weight bis-trifluoromethyl-pyrazole (BTP) derivative originally developed by Abbott Laboratories as a novel, calcineurin-independent inhibitor of the Nuclear Factor of Activated T cells (NFAT) transcription factor family. It acts by maintaining NFAT in a phosphorylated state in the cytosol, thereby blocking its nuclear translocation and subsequent transcription of NFAT-dependent genes, without affecting calcineurin phosphatase activity, NF-κB, or AP-1 activation. Although initially investigated as a safer immunosuppressive agent, its clinical development was discontinued due to severe side effects, including neurotoxicity. However, A-285222 remains widely used as a research tool to study the role of NFAT signaling in various pathological conditions, such as diabetic microvascular and macrovascular complications, atherosclerosis, and pulmonary arterial hypertension.

Other names

compound 19compound19compound-19