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Chemical Structure : MPK5 inhibitor 1
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.
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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.
| M.Wt | 364.54 | |
| Formula | C17H20N2OS3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Zachary T K Gannam, et al. Sci Signal. 2020 Aug 25;13(646):eaba3043.
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