||MIM 1;MIM-1;Inhibitor of Mcl-1; 4-((E)-(((Z)-2-(cyclohexylimino)-4-methylthiazol-3(2H)-yl)imino)methyl)benzene-1,2,3-triol
MIM1 is a selective small molecule inhibitor of Mcl-1(IC50= 4.8 uM) that overcomes Mcl-1-dependent leukemia cell survival.
IC50 value: 4.8 uM
MIM1 effectively competed with FITC-MCL-1 SAHBA and FITC-BID BH3 for MCL-1ΔNΔC binding with respective IC50s of 4.7 and 4.8 μM, the compound showed no capacity to displace FITC-BID BH3 from BCL-XLΔC (IC50>50 μM), mirroring the selectivity of MCL-1 SAHBD.
Although MCL-1 SAHBD was a 30 to 60-fold more potent competitor for MCL-1ΔNΔC binding than MIM1, the MCL-1 selective small molecule is one-seventh the size of the stapled peptide and exhibits an IC50 for its target (4.8 μM) that is only 7.5-fold less than that of chemically-optimized ABT-737 for BCL-XLΔC (0.63 μM) upon competition with FITC-BID BH3.
Protocol(Only for Reference)
Physical and Chemical Properties
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Mechanism and Indication
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