BML-260 (BML260) is a potent inhibitor of dual-specific phosphatase JSP-1 (JNK Stimulatory Phosphatase-1, DUSP22) and stimulator of uncoupling protein 1 (UCP-1) expression in adipocytes.
BML-260 activates UCP1 expression (both the mRNA level and the protein level) and increases mitochondrial activity in brown adipocytes.
BML-260 stimulates the expression of UCP1 in adipocytes in a JSP-1 independent manner.
BML-260 upregulates thermogenic and muscle program genes.
BML-260 induces UCP1 expression in white adipocytes and enhances thermogenesis, activates UCP1 and increases thermogenesis in vivo.
JSP-1 is a dual-specific phosphatase encoded by DUSP22 (dual specificity phosphatase 22), which is also known as JKAP (JNK pathway-associated phosphatase), JSP-1 is a JNK activator, and a proposed target for the treatment of inflammatory and proliferative disorders associated with dysfunctional JNK signaling.