Catalog No.: PC-72803Not For Human Use, Lab Use Only.
MPK5 inhibitor 1 (MPK5-IN-1, MPK5 inhibitor compound 1) is a potent, selective allosteric inhibitor of MAPK phosphatase MKP5 with Kd/IC50 of 1.0/3.9 uM.
MPK5 inhibitor 1 (MPK5-IN-1, MPK5 inhibitor compound 1) is a potent, selective allosteric inhibitor of MAPK phosphatase MKP5 with Kd/IC50 of 1.0/3.9 uM.
MPK5 inhibitor 1 also inhibited the full-length MKP5 with similar potency to the catalytic domain, showed little to no inhibition on STEP-46, PTP-1B and other members of the MKP family, MKP1, MKP3, and MKP7 (IC50>100 uM).
MPK5 inhibitor 1 also inhibited Y435W mutant with Kd/IC50 of 1.3/2.9 uM, but not for mutants Y435A/Y435S/T432D/M431L-T432D, suggesteTyr435 as essential for phosphatase activity of MPK5.
MPK5 inhibitor 1 induces MAPK activity and stimulates myoblast differentiation, MKP5 is required for TGF-β1 signaling and MPK5 inhibitor 1 inhibits Smad2 activity.
MKP5 targeting may serve as a therapeutic pathway for the treatment of dystrophic muscle disease.
