| Identification | Back Directory | [Name]
MM-102 | [CAS]
1417329-24-8 | [Synonyms]
MM-102
CS-2007
MM-102 TFA Salt
MM-102 USP/EP/BP
HMTase Inhibitor IX
HMTASE INHIBITOR IX;MM102;MM 102;MM-102
1-[[(2S)-5-[(Aminoiminomethyl)amino]-2-[[2-ethyl-2-[(2-methyl-1-oxopropyl)amino]-1-oxobutyl]amino]-1-oxopentyl]amino]-N-[bis(4-fluorophenyl)methyl]cyclopentanecarboxamide]
Cyclopentanecarboxamide, 1-[[(2S)-5-[(aminoiminomethyl)amino]-2-[[2-ethyl-2-[(2-methyl-1-oxopropyl)amino]-1-oxobutyl]amino]-1-oxopentyl]amino]-N-[bis(4-fluorophenyl)methyl]- | [Molecular Formula]
C35H49F2N7O4 | [MDL Number]
MFCD28015099 | [MOL File]
1417329-24-8.mol | [Molecular Weight]
669.8 |
| Chemical Properties | Back Directory | [density ]
1.26±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20° C | [solubility ]
insoluble in H2O; ≥22.6 mg/mL in EtOH; ≥67 mg/mL in DMSO | [form ]
Powder | [pka]
12.90±0.20(Predicted) |
| Hazard Information | Back Directory | [Uses]
MM-102 is a small molecule WDR5/MLL1 protein-protein interaction inhibitor. MM-102 in bone marrow cells transduced with MLL1-AF9 fusion construct decreases the expression of HoxA9 and Meis-1, two critical MLL1 target genes in MLL1 fusion protein mediated leukemogenesis. | [Biological Activity]
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]. | [target]
MLL1 | [storage]
Store at -20° C | [References]
[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. |
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