MM-102

MM-102

Catalog Number:
L002370110APE
Mfr. No.:
APE-B1582
Price:
$209
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      • Overview
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          Background

          MM-102 is an antagonist of MLL1 with IC50 value of 2.4nM [1].
          Mixed lineage leukemia 1 (MLL1) is a histone H3 lysine 4 (H3K4) methyltransferase. The interaction of MLL1 and WDR5 is essential for MLL1 enzymatic activity and is a target for the treatment of acute leukemia. MM-102 is a peptidomimetic of MLL1. It has a high binding affinity to WDR5 with IC50 value of 2.4nM [1].
          MM-102 is reported to reduce the expression of MLL1 targeted genes HoxA9 and Meis-1 in MLL1-AF9 transduced murine cells. Since these two genes are required for MLL1 mediated leukemogenesis, MM-102 is found to inhibit cell growth of leukemia cells harboring MLL1 fusion proteins. It dose-dependently inhibits the cell growth in the MV4;11 and KOPN8 cell lines with IC50 values both of 25μM[1].

          [1] Karatas H, Townsend EC, Cao F, Chen Y, Bernard D, Liu L, Lei M, Dou Y, Wang S. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. J Am Chem Soc. 2013 Jan 16;135(2):669-82.

      • Properties
        • Alternative Name
          N-[bis(4-fluorophenyl)methyl]-1-[[(2S)-5-(diaminomethylideneamino)-2-[[2-ethyl-2-(2-methylpropanoylamino)butanoyl]amino]pentanoyl]amino]cyclopentane-1-carboxamide
          CAS Number
          1417329-24-8
          Molecular Formula
          C35H49F2N7O4
          Molecular Weight
          669.8
          Purity
          98.00%
          Solubility
          insoluble in H2O; ≥22.6 mg/mL in EtOH; ≥67 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Li N, Yang L, et al. "BET bromodomain inhibitor JQ1 preferentially suppresses EBV-positive nasopharyngeal carcinoma cells partially through repressing c-Myc." Cell Death Dis. 2018 Jul 9;9(7):761. PMID:29988031

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