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MM-102
CAS No. : 1417329-24-8
Biological Activity：MM-102 (HMTase Inhibitor IX) is a potent WDR5/MLL interaction inhibitor, achieves IC50= 2.4 nM with an estimated Ki< 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
IC50 value: 2.4 nM
Target: MLL
in vitro: MM-102 inhibits MLL1 methyltransferase activity and MLL-1-induced HoxA9 and Meis-1 gene expression in leukemia cells expressing the MLL1-AF9 fusion gene. Also inhibits cell growth and induces apoptosis in leukemia cells harbouring MLL1 fusion proteins. MM-102, with the highest binding affinities to WDR5, also show the most potent inhibitory activity in the HMT assay with IC50 = 0.4-0.9 μM. MM-102 dose-dependently inhibits cell growth in the MV4;11 and KOPN8 leukemia cell lines, which carry MLL1-AF4 and MLL1-ENL fusion proteins, respectively. MM-102 has IC50 = 25 μM in both cell lines and completely inhibits cell growth in these cell lines at 75 μM. MM-102 effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins and has minimal effect in leukemia cells with wild-type MLL1 protein.[1]
Research Area：Cancer
Targets：Histone Methyltransferase
Related Small Molecules:EEDi-5285;EZH2-IN-2;BIX-01294;SGC707;(S)-HH2853;G9a-IN-1;UNC4976;MS1943;OTS186935 hydrochloride;MS8815;(R)-HH2853;EPZ020411;Furamidine dihydrochloride;EZH2-IN-12;UNC0642;MU1656;Chaetocin;UNC0646;UNC0224;MRK-740;SMYD2-IN-1;PRMT5-IN-21;Sinefungin;MM-401;SETDB1-TTD-IN-1;Dot1L-IN-2;PRMT5-IN-10;PRMT1-IN-1
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