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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-MTX115325
MTX115325

Chemical Structure : MTX115325

CAS No.: 2750896-25-2

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MTX115325 (MTX-115325, MTX 115325)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 348.37
分子式 C18H16N6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

参考文献

1. Patent WO 2021/249909 A1.

2. Fang TZ, et al. Nat Commun. 2023 Nov 13;14(1):7295.

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