Mcl-1-IN-22

Mcl-1-IN-22 (Compound N5) potently and selectively binds to purified Mcl-1 protein with a K_i of 0.015 μM, and exhibits minimal binding to Bcl-2, Bcl-xL, Bcl-w, and Bfl-1^[1].
Mcl-1-IN-22 potently inhibits proliferation of Mcl-1-dependent A2780S, HO8910, H929, and MV411 cancer cells, has weak activity against ARH-77 cells, no activity against OVCAR3 cells, and low toxicity to normal HL-7702 and WI-38 cells^[1].
Mcl-1-IN-22 (6 μM; 18 h) binds to intracellular Mcl-1 in A2780S cells, increasing the protein's thermal stability by raising its melting temperature by over 10 °C^[1].
Mcl-1-IN-22 (3-6 μM) disrupts Bak-Mcl-1 complexes in A2780S cells in vitro in a concentration-dependent manner, increasing levels of free Bak^[1].
Mcl-1-IN-22 (3-6 μM) induces apoptosis in A2780S cells in vitro in a concentration-dependent manner, with robust activation of caspase-9 and caspase-3 that exceeds the activity of AZD5991 at matching concentrations^[1].
Mcl-1-IN-22 maintains potent antiproliferative activity against Cisplatin (HY-17394)-resistant A2780/CDDP cells, but its activity is dependent on Mcl-1 expression^[1].
Mcl-1-IN-22 acts synergistically with Cisplatin and Paclitaxel (HY-B0015) to inhibit proliferation of A2780S and Cisplatin-resistant A2780/CDDP cells, with the strongest synergy observed with Paclitaxel in A2780/CDDP cells (CI = 0.4)^[1].
Mcl-1-IN-22 (200 nM) does not exhibit significant binding affinity or inhibitory activity against HDAC 3, HDAC 4, HDAC 6, or HDAC 11 proteins^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.