Mcl-1 Inhibitor II-Calbiochem

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一般描述

A cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8 nM FITC-AHA-BIM_142-161for Mcl-1, but not Bcl-xL, binding (IC₅₀= 310 nM vs >40 ?M; [Mcl-1] & [Bcl-xL] = 6.25 nM), displaying little inhibitory potency toward CYP450 isoforms 1A2/2D6/3A4/2C9 (IC₅₀= >10 ?M). Antiproliferation potencies against 2 murine lymphoma cell lines (GI₅₀= 300 nM/ MCl1-1780 & 1.1 ?M/Bcl2-1863) and 11 human cancer lines of various origins (GI₅₀from 1.6 to 25 ?M) correlate well with intracellular BH3 domain peptide-binding capacity. Likewise, greater apoptosis induction is observed in MCl1-1780 than the highly Bcl-2/Bcl-xL primed Bcl2-1863 cultures upon drug treatment. Stability studies using murine and human liver microsome preparations revealt_1/2values of 40 min and 55 min, respectively.
A cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8 nM FITC-AHA-BIM_142-161for Mcl-1, but not Bcl-xL, binding (IC₅₀= 310 nM vs >40 ?M; [Mcl-1] & [Bcl-xL] = 6.25 nM). Antiproliferation potencies against 2 murine lymphoma cell lines and 11 human cancer lines of various origins (GI₅₀from 0.3 to 25 ?M) correlate well with intracellular BH3 domain peptide-binding capacity. Likewise, greater apoptosis induction is observed in MCl1-1780 than the highly Bcl-2/Bcl-xL primed Bcl2-1863 cultures upon drug treatment.

生化/生理作用

Cell permeable: yes
Reversible: yes
Primary Target
Mcl-1

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他说明

Richard, D.J., et al. 2013.Bioorg. Med. Chem.21,6642.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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