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

Mcl-1 Inhibitor III, UMI-77 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Myeloid 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

Primary Target: binds to the BH3 binding groove of Mcl-1
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₈H₁₄BrNO₅S₂
Description
Overview

This product has been discontinued.



A 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
Global Trade Item Number
Catalogue Number GTIN
509266 0

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 Protect from light
+2°C to +8°C
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.