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MilliporeSigma™ Calbiochem™ Mcl-1 Inhibitor II

Catalog No. 5080530001 Shop All MilliporeSigma Products
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10mg

Description

A cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8nM FITC-AHA-BIM142-161 for Mcl-1, but not Bcl-xL, binding (IC50 = 310nM vs >40μM; [Mcl-1] & [Bcl-x

A cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8nM FITC-AHA-BIM142-161 for Mcl-1, but not Bcl-xL, binding (IC50 = 310nM vs >40μM; [Mcl-1] & [Bcl-xL] = 6.25nM), displaying little inhibitory potency toward CYP450 isoforms 1A2/2D6/3A4/2C9 (IC50 = >10μM). Antiproliferation potencies against 2 murine lymphoma cell lines (GI50 = 300 nM/ MCl1-1780 & 1.1μM/Bcl2-1863) and 11 human cancer lines of various origins (GI50 from 1.6 to 25μM) 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 reveal t 1/2 values of 40 min and 55 min, respectively.
TRUSTED_SUSTAINABILITY

Specifications

Color White
Description 95% by HPLC
Target Proteins Mcl-1
Molecular Formula C23H24F3N3O
Solubility DMSO
Content And Storage Protect from light
Form Powder
Quantity 10 mg
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