MM-102  (Synonyms: HMTase Inhibitor IX)

MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC₅₀=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos^{[1][2][3][4][5]}.

MM-102 (40 µM; 4 d) induces growth arrest and cell death in MLL1-AF9-transformed mouse leukemia cells specifically in leukemia cells harboring the MLL1 translocation, but does not interfere with the growth of normal bone marrow^[2].
MM-102 (2, 10, and 50 µM) disrupts the association of WDR5 and RbBP5 with GSTMLL1 in a concentration-dependent manner. The association of WDR5 with MLL1 is mildly disrupted at 2 µM, moderately disrupts at 10 µM, and completely disrupts at 50 µM^[2].
MM-102 specifically inhibits the methyltransferase activity of the MLL1 complex with an IC₅₀ value of 0.32 µM^[2].
MM-102 (50 µM; 48 h) can significantly inhibit the proliferation, migration and chemoresistance of TFK1 and RBE cells^[3].
MM-102 (50 µM; 1 h) not only significantly reduces the expression of MLL1, WDR5 and H3K4me3 in TGF-b1-stimulated NRK-49F cells, but also inhibits the expression of p16INK4a^[4].
MM-102 (50-100 μM; 48 h) enhances the developmental competence of porcine SCNT embryos and improves the expression pattern of key genes in SCNT embryo development^[5].

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

MM-102 (15 mg/kg; i.p.; once daily for 7 days) inhibits tumor progression in primary CCA model mice^[3].
MM-102 (15 mg/kg; i.p.; once daily for 7 days) inhibits p16INK4a gene expression in IRI mice and reduces renal fibrosis and renal inflammation in IRI mice^[4].

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

669.80

C₃₅H₄₉F₂N₇O₄

1417329-24-8

Solid

White to off-white

O=C(C1(NC([C@@H](NC(C(NC(C(C)C)=O)(CC)CC)=O)CCCNC(N)=N)=O)CCCC1)NC(C2=CC=C(F)C=C2)C3=CC=C(F)C=C3

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Karatas H, et al. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. J Am Chem Soc. 2013, 135(2), 669-682.  [Content Brief]

  [2]. Townsend E C. Development of a Novel Inhibitor to the Conserved, Developmental Regulator, WDR5, for Treatment of Acute Leukemia[D]. , 2012.

  [3]. Wang D, et al. MBD2 regulates the progression and chemoresistance of cholangiocarcinoma through interaction with WDR5[J]. Journal of Experimental & Clinical Cancer Research, 2024, 43(1): 272.  [Content Brief]

  [4]. Hara D, et al. Inhibition of H3K4 Trimethylation Ameliorates Peritoneal Fibrosis and Senescence: FR-PO456[J]. Journal of the American Society of Nephrology, 2022, 33(11S): 447-448.  [Content Brief]

  [5]. Zhang Z, et al. Down-regulation of H3K4me3 by MM-102 facilitates epigenetic reprogramming of porcine somatic cell nuclear transfer embryos[J]. Cellular Physiology and Biochemistry, 2018, 45(4): 1529-1540.  [Content Brief]