2,5-Dimethyl-celecoxib

White solid. Soluble in DMSO, methanol or dichloromethane. Close structural analog of the selective cyclooxygenase-2 (COX-2) inhibitor celecoxib, that lacks COX-2 inhibitory function, Anti-proliferative, anti-tumorigenic and anti-angiogenic, Potent apoptosis inducer in many cancer cell lines, Down-regulates the expression of survivin, cyclins, MMPs and inhibits cyclin-dependent kinase activity, Modulates PDK-1, AKT, GSK3beta, p70 S6K, PKA and MAPKAP-K1alpha, Reduces phosphorylation of ERK1/2 but not AKT T-308 or AKT S-473, Increases intracellular free calcium levels and potently triggers the endoplasmatic reticulum stress response (ESR), activating ER stress-associated proteins GRP78/BiP, CHOP/GADD153 and caspase-4.