UMI-77

- Overview
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    Background
    
    UMI-77 is a novel small-molecule inhibitor of Mcl-1 with Ki and IC50 values of 0.49 μM and 0.31 μM [1].
    Myeloid cell leukemia-1 (Mcl-1) is a member of the prosurvival Bcl-2 family and is a potent anti-apoptotic protein. Mcl-1 acts as an important survival factor in a broad range of human cancers [1].
    UMI-77 is a novel small-molecule Mcl-1 inhibitor. In FP-based binding assays, UMI-77 potently and selectively displaced fluorescent labeled BID-BH3 peptide from Mcl-1 protein with Ki value of 0.49μM and bound to the BH3 binding pocket of Mcl-1 protein. UMI-77 bound to A1/Bfl-1, Bcl-w, Bcl-2 and Bcl-xL with Ki values of 5.33, 8.19, 23.83 and 32.99μM. In a pull-down assay, UMI-77 at 10 μM effectively and dose-dependently inhibited the interactions between BL-Noxa and cellular Mcl-1. It was reported that Mcl-1 regulates pro-apoptotic Bax and Bak proteins and preventing their pro-apoptotic activity. UMI-77 dose-dependently inhibited the binding of Mcl-1 to Bax with IC50 value of 1.43μM. In PC cells, UMI-77 inhibited cell growth and induced apoptosis in a time and dose-dependent way [1].
    In BxPC-3 xenografted SCID mice model, UMI-77 exhibited robust anti-tumor efficacy with no toxicity. Also, UMI-77 decreased the anti-apoptotic protein survivin, which potently inhibited apoptosis by antagonizing caspase activity [1].
- Properties
  - Alternative Name
    
    2-[4-[(4-bromophenyl)sulfonylamino]-1-hydroxynaphthalen-2-yl]sulfanylacetic acid
    
    CAS Number
    
    518303-20-3
    
    Molecular Formula
    
    C18H14BrNO5S2
    
    Molecular Weight
    
    468.34
    
    Appearance
    
    A solid
    
    Purity
    
    98.03%
    
    Solubility
    
    ≥23.4 mg/mL in DMSO; insoluble in H2O; ≥7.2 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Robinson EJ, Aguiar SP, et al. "Survival of midbrain dopamine neurons depends on the Bcl2 factor Mcl1." Cell Death Discov. 2018 Nov 21;4:107. PMID:30479840

UMI-77

Background

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