欢迎访问ProbeChem中文网站，英文网站请访问www.probechem.com
    英文 |     中文

产品咨询: sales@probechem.com
订购: order@probechem.com

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

Chemical Structure : MTX115325

CAS No.: 2750895-97-5

加入收藏

MTX115325 (MTX325, MTX-325)

货号: PC-21351Not For Human Use, Lab Use Only.

MTX115325 (MTX325, MTX-325) is a potent, selective, brain-penetrant USP30 inhibitor with IC50 of 12 nM in biochemical fluorescence polarization assays.

规格 价格 库存 数量
25 mg Get quote
50 mg Get quote
100 mg Get quote
获取报价单
* 请选择数量再加入购物车
 or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    MTX115325 (MTX325, MTX-325) 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

    (3aR,4R,6aR)-1-(5-(2-cyanopyridin-4-yl)oxazole-2-carbonyl)-4-methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carbonitrile

    参考文献

    1. Patent WO 2021/249909 A1.

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

    备案号：沪ICP备16042516号-1 Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

    联系我们 sales@probechem.com

    Bulk Inquiry

    * Indicates a Required FieldYour information is safe with us.

    • *Product name:
    • *Applicant name:
    • *Email address:
    • *Organization name:
    • *Requested quantity:
    • *Country:
    • *Additional Information:

    询单

    • *产品名称:
    • *姓名:
    • *邮箱:
    • *公司名称:
    • *询单数量:
    • *国籍:
    • 询单信息: