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MM-102 TFA

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Chemical Structure
1883545-52-5
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More than 5000 active chemicals with high quality for research!
Field of application
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
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1883545-52-5
Chemical Name: MM-102 TFA
Synonyms: MM-102 TFA;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]-cyclopentanecarboxamidetrifluoroacetate;N-[bis(4-fluorophenyl)methyl]-1-[[(2S)-5-(diaminomethylideneamino)-2-[[2-ethyl-2-(2-methylpropanoylamino)butanoyl]amino]pentanoyl]amino]cyclopentane-1-carboxamide;2,2,2-trifluoroacetic acid;MM 102;HMTase Inhibitor IX TFA;EX-A;MM-102 (Tfa)
SMILES: FC1C=CC(=CC=1)C(C1C=CC(=CC=1)F)NC(C1(CCCC1)NC([C@H](CCC/N=C(\N)/N)NC(C(CC)(CC)NC(C(C)C)=O)=O)=O)=O.FC(C(=O)O)(F)F
Formula: C37H50F5N7O6
M.Wt: 783.828226566315
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: MM-102 (HMTase Inhibitor IX) TFA is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
Target: IC50: 2.4 nM (MLL)[1].
In Vitro: 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 with IC50 = 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].
Cell Assay: MV4;11, KOPN8, and K562 cells were cultured in RPMI 1640 medium (ATCC) supplemented with 10% fetal bovine serum and 100 U/L penicillinstreptomycin and incubated at 37°C under 5% CO2. Cells were seeded into 12-well plates for suspension at a density of 5 × 105 per well (1 mL) and treated with either vehicle control (DMSO, 0.2%) or MM-102 (HMTase Inhibitor IX) for 7 days. The medium was changed every 2 days, and compounds were resupplied. The CellTiter-Glo Luminescent Cell Viability Assay kit was used. First, 100 μL of the assay reagent was added into each well, and the content was mixed for 2 min on an orbital shaker to induce cell lysis. After 10 min incubation at room temperature, the luminescence was read on a microplate reader.
References: [1]. Karatas H, et al. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. J Am Chem Soc. 2013 Jan 16;135(2):669-682.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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