An inhibitor of WDR5/MLL interactions
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MM-102

Item No. 17699

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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
CAS Number
1417329-24-8
Molecular Formula
C35H49F2N7O4
Formula Weight
669.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 25 mg/mlEthanol: 20 mg/ml
SMILES
NC(NCCC[C@@H](C(NC1(CCCC1)C(NC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)=O)=O)NC(C(CC)(CC)NC(C(C)C)=O)=O)=N
InChi Code
InChI=1S/C35H49F2N7O4/c1-5-34(6-2,43-29(45)22(3)4)31(47)41-27(10-9-21-40-33(38)39)30(46)44-35(19-7-8-20-35)32(48)42-28(23-11-15-25(36)16-12-23)24-13-17-26(37)18-14-24/h11-18,22,27-28H,5-10,19-21H2,1-4H3,(H,41,47)(H,42,48)(H,43,45)(H,44,46)(H4,38,39,4
InChi Key
RZKSQRIPRKWVBU-MHZLTWQESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $253

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    25 mg

    $587

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    Cayman Chemical
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    Product Description

    WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.1 It serves as a component of a mixed-lineage leukemia (MLL) methyltransferase complex that targets histone 3 at lysine 4 to upregulate transcription.2 MM-102 is a potent WDR5/MLL interaction inhibitor (IC50 = 2.4 nM).3 It has been shown to block MLL1 methyltransferase activity, reducing the expression of HoxA9 and Meis-1 genes, which are both critical MLL1 target genes in MLL1 fusion protein-mediated leukemogenesis.3 MM-102 can also inhibit cell growth and induce apoptosis in leukemia cells harboring MLL1 fusion proteins.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Migliori, V., Mapelli, M., and Guccione, E. On WD40 proteins: Propelling our knowledge of transcriptional control? Epigenetics 7(8), 815-822 (2012).

    2. Guccione, E., Bassi, C., Casadio, F., et al. Methylation of histone H3R2 by PRMT6 and H3K4 by an MLL complex are mutually exclusive. Nature 449(7164), 933-937 (2007).

    3. Karatas, H., Townsend, E.C., Cao, F., et al. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. J. Am. Chem. Soc. 135(2), 669-682 (2013).

    Product Citations

    Yang, B., Alimperti, S., Gonzalez, M.V., et al. Reepithelialization of diabetic skin and mucosal wounds is rescued by treatment with epigenetic inhibitors. Diabetes 73(1), 120-134 (2024).