MilliporeSigma™ Calbiochem™ Mcl-1 Inhibitor II

Description

• A cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8nM FITC-AHA-BIM 142-161 for Mcl-1, but not Bcl-xL, binding (IC 50 = 310nM vs >40μM; [Mcl-1] & [Bcl-xL] = 6.25nM), displaying little inhibitory potency toward CYP450 isoforms 1A2/2D6/3A4/2C9 (IC 50 = >10μM)
• Antiproliferation potencies against 2 murine lymphoma cell lines (GI 50 = 300 nM/ MCl1-1780 & 1.1μM/Bcl2-1863) and 11 human cancer lines of various origins (GI 50 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.