509266 Mcl-1 Inhibitor III, UMI-77 - Calbiochem

509266
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₈H₁₄BrNO₅S₂

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable, bioavailable hydroxynaphthalenylthioacetate compound that selectively and reversibly binds to the BH3 binding groove of Mcl-1 (Ki = 490 nM) and antagonizes its function by disrupting the heterodimerization of Mcl-1/Bax (IC50 = 1.43 µM) and Mcl-1/Bak in cells. Exhibits high selectivity over other members of the Bcl-2 family (Ki = 5.33, 8.19, 23.83, and 32.99 µM, for A1/Bfl-1, Bcl-w, Bcl-2, and Bcl-xL, respectively). Inhibits the growth of BxPC-3, Panc-1 cells, and Capan-2 cells (IC50 = 3.4, 4.4, and 5.5 µM, respectively) by inducing intrinsic apoptosis as evidenced by cytochrome c release and caspase-3 activation. However, it does not induce apoptosis in normal cells. Blocks the growth of BxPC-3 xenograft in SCID mice (60 mg/kg i.v. for 5 days for 2 weeks) without any cytotoxic effects on surrounding normal tissue. Exhibits desirable microsomal stability (t1/2 = 45 min. in murine models).
      Catalogue Number509266
      Brand Family Calbiochem®
      SynonymsMyeloid Cell Leukemia-1 Inhibitor III, UMI77, 2-(4-(4-Bromophenylsulfonamido)-1-hydroxynaphthalen-2-ylthio)acetic acid, ((4-(((4-Bromophenyl)sulfonyl)amino)-1-hydroxy-2-naphthyl)sulfanyl)acetic acid
      References
      ReferencesAbulwerdi, F., et al. 2014. Mol. Cancer Ther. 13, 565.
      Product Information
      FormOff-white solid
      Hill FormulaC₁₈H₁₄BrNO₅S₂
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetbinds to the BH3 binding groove of Mcl-1
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Mcl-1 Inhibitor III, UMI-77 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Abulwerdi, F., et al. 2014. Mol. Cancer Ther. 13, 565.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision01-March-2016 JSW
      SynonymsMyeloid Cell Leukemia-1 Inhibitor III, UMI77, 2-(4-(4-Bromophenylsulfonamido)-1-hydroxynaphthalen-2-ylthio)acetic acid, ((4-(((4-Bromophenyl)sulfonyl)amino)-1-hydroxy-2-naphthyl)sulfanyl)acetic acid
      DescriptionA cell-permeable hydroxynaphthalenylthioacetate that exhibits Mcl-1-selective affinity (Ki against 2 nM FITC-BID79-99 binding = 490 nM/90 nM MCl-1 & 23.83 µM/60 nM Bcl-2; Ki against 1 nM FAM-BID80-99 binding = 5.33 µM/4 nM A1/Bfl-1; Ki against 2 nM FAM-BID80-99 binding = 8.19 µM/40 nM Bcl-w, 23.83 µM/60 nM Bcl-2, and 32.99 µM/50 nM Bcl-xL), effectively inhibiting Mcl-1 BH3-binding groove-mediated interactions with various binding partners, including Noxa, Bax, and Bak, by simultaneously targeting the groove′s h2 & h3 hydrophobic pockets. Shown to inhibit the proliferation of BxPC-3, Panc-1, and Capan-2 prostate cancer cultures (IC50 = 3.4, 4.4, and 5.5 µM, respectively) via apoptosis induction, while being less potent toward MiaPaca and AsPC-1 lines (IC50 = 12.5 and 16.1 µM, respectively) with high Bcl-xL and low Mcl-1/Bak expression and. Despite its moderate in vitro murine liver microsome stability (t1/2 = 45 mins), daily i.v. injection (60 mg/kg; 5 d/wk) is reported to effectively suppress BxPC-3 tumor expansion in mice in vivo without apparent animal toxicity, although severe weight loss is observed among mice received higher daily MUI-77 i.v. dosage of 80 mg/kg.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Purity≥98% by HPLC
      SolubilityDMSO (10 mg/ml). Use only fresh DMSO for reconstitution.
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesAbulwerdi, F., et al. 2014. Mol. Cancer Ther. 13, 565.