MM-102 is a Potent WDR5/MLL interaction inhibitor. The MM-102 compound prevents the interaction between mixed lineage leukemia 1 (MLL1) and WD Trp-Asp repeat domain 5 (WDR5) and results in the inhibition of MLL1 H3K4 histone methyltransferase (HMT) activity. Down-Regulation of H3K4me3 by MM-102 Facilitates Epigenetic Reprogramming of Porcine Somatic Cell Nuclear Transfer Embryos
Chemical Formula: C37H50F5N7O6
Molecular Weight: 783.842
Elemental Analysis: C, 56.70; H, 6.43; F, 12.12; N, 12.51; O, 12.25
MM-102 trifluoroacetic acid
Smiles Code: 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.O=C(O)C(F)(F)F
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
MM-102 (HMTase Inhibitor IX) 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 (TFA), with the highest binding affinities to WDR5, also show the most potent inhibitory activity in the HMT assay withIC50=0.4-0.9 μM.
MM-102 (HMTase Inhibitor IX) 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 (HMTase Inhibitor IX) has IC50=25 μM in both cell lines and completely inhibits cell growth in these cell lines at 75 μM.
MM-102 (HMTase Inhibitor IX) 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.Han X, Xiang J, Li C, Wang J, Wang C, Zhang Y, Li Z, Lu Z, Yue Y, Li X. MLL1 combined with GSK3 and MAP2K inhibition improves the development of in vitro- fertilized embryos. Theriogenology. 2020 Apr 1;146:58-70. doi: 10.1016/j.theriogenology.2020.01.051. Epub 2020 Jan 29. PMID: 32059151.
Shimoda H, Doi S, Nakashima A, Sasaki K, Doi T, Masaki T. Inhibition of the H3K4 methyltransferase MLL1/WDR5 complex attenuates renal senescence in ischemia reperfusion mice by reduction of p16INK4a. Kidney Int. 2019 Nov;96(5):1162-1175. doi: 10.1016/j.kint.2019.06.021. Epub 2019 Aug 1. PMID: 31570196.
Zhang Z, Zhai Y, Ma X, Zhang S, An X, Yu H, Li Z. Down-Regulation of H3K4me3 by MM-102 Facilitates Epigenetic Reprogramming of Porcine Somatic Cell Nuclear Transfer Embryos. Cell Physiol Biochem. 2018;45(4):1529-1540. doi: 10.1159/000487579. Epub 2018 Feb 16. PMID: 29466785.
Weirich S, Kudithipudi S, Jeltsch A. Somatic cancer mutations in the MLL1 histone methyltransferase modulate its enzymatic activity and dependence on the WDR5/RBBP5/ASH2L complex. Mol Oncol. 2017 Apr;11(4):373-387. doi: 10.1002/1878-0261.12041. Epub 2017 Mar 10. PMID: 28182322; PMCID: PMC5527479.
Cai M, Bompada P, Atac D, Laakso M, Groop L, De Marinis Y. Epigenetic regulation of glucose-stimulated osteopontin (OPN) expression in diabetic kidney. Biochem Biophys Res Commun. 2016 Jan 1;469(1):108-113. doi: 10.1016/j.bbrc.2015.11.079. Epub 2015 Nov 22. PMID: 26592666.
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