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Chemical Structure : MTX115325
Catalog No.: PC-21351Not For Human Use, Lab Use Only.
MTX115325 is a potent, selective, brain-penetrant USP30 inhibitor with IC50 of 12 nM in biochemical fluorescence polarization assays.
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MTX115325 is a potent, selective, brain-penetrant USP30 inhibitor with IC50 of 12 nM in biochemical fluorescence polarization assays.
MTX115325 exhibits high selectivity (>2000-fold) against 54 DUBs and other cysteinyl proteases.
MTX115325 blocks access of a ubiquitin-like probe to the enzyme active site in cells with IC50 of 25 nM.
MTX115325 increases ubiquitylation of the outer mitochondrial membrane protein TOM20, a USP30 substrate, with an EC1.5x and EC50 of 10 nM and 32 nM respectively, in human HeLa cell line overexpressing PARKIN and challenged with the mitochondrial toxins antimycin A and oligomycin A (A/O).
MTX115325 treatment (10 nM-1 uM) causes the upregulation of TOM20-ubiquitylation in human dopaminergic neurons in vitro, without any exogenous stimuli.
MTX115325 potently inhibits mouse USP30 with an IC50 of 13 nM, similar to human USP30.
MTX115325 (50 mg/kg BID, oral gavage) prevents dopaminergic neuronal loss and dopamine depletion in an α-synuclein-based PD mouse model.
MTX115325 recapitulates the effects of Usp30 KO in protecting against TH+ neuronal loss and striatal dopamine loss in an αSyn-based PD mouse model.
| M.Wt | 348.37 | |
| Formula | C18H16N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Patent WO 2021/249909 A1.
2. Fang TZ, et al. Nat Commun. 2023 Nov 13;14(1):7295.
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