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MM-102 TFA

Catalog No. T8768   CAS 1883545-52-5
Synonyms: HMTase Inhibitor IX TFA

MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM. 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 Embry

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MM-102 TFA Chemical Structure
MM-102 TFA, CAS 1883545-52-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 33.00
2 mg In stock $ 47.00
5 mg In stock $ 107.00
10 mg In stock $ 177.00
25 mg In stock $ 298.00
50 mg In stock $ 443.00
100 mg In stock $ 653.00
1 mL * 10 mM (in DMSO) In stock $ 152.00
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Purity: 99.4%
Purity: 99.3%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM. 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 Embry
Targets&IC50 MLL1:0.4 μM
In vitro MM-102, in bone marrow cells transduced with MLL1-AF9 fusion construct shows that the compound effectively decreases the expression of HoxA9 and Meis-1, two critical MLL1 target genes in MLL1 fusion protein mediated leukemogenesis.?MM-102 also specifically inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins.
Kinase Assay In Vitro Histone Methyltransferase (HMT) Assay: The HMT assay is performed in 50 mM HEPES pH 7.8, 100 mM NaCl, 1.0 mM EDTA, and 5% glycerol at 22 °C. Each reaction contains 1.5 μCi of the co-factor, 3H-S-adenosylmethionine. H3 10-residue peptide is used as the substrate at 50 μM. Compounds are added at concentrations ranging from 0.125 to 128 μM and incubated with the pre-assembled WDR5/RbBP5/ASH2L complex at a final concentration of 0.5 μM for each protein for 2–5 min. Reactions are initiated by addition of the MLL1 protein at a final concentration of 0.5 μM and allowed to proceed for 30 min before preparing scintillation counting. To count samples, reactions are spotted on separate squares of P81 filter paper and precipitated by submerging in freshly prepared 50 mM sodium bicarbonate buffer with pH 9.0. After washing and drying, samples are vortexed in Ultima Gold scintillation fluid and counted. As a negative control, assays are performed using 0.5 μM MLL1/WDR5/RbBP5/ASH2L complex assembled with the non-interacting mutant, WDR5D107A.
Synonyms HMTase Inhibitor IX TFA
Molecular Weight 783.83
Formula C37H50F5N7O6
CAS No. 1883545-52-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 99 mg/mL(126.3 mM)

TargetMolReferences and Literature

1. Karatas H, et al. J Am Chem Soc. 2013, 135(2), 669-682.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Reprogramming Compound Library Bioactive Compounds Library Max Epigenetics Compound Library Stem Cell Differentiation Compound Library PPI Inhibitor Library Chromatin Modification Compound Library Bioactive Compound Library Histone Modification Compound Library Methylation Compound Library

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Keywords

MM-102 TFA 1883545-52-5 Chromatin/Epigenetic Histone Methyltransferase MM102 HMTase Inhibitor IX TFA HMTase Inhibitor IX MM-102 MM 102 TFA MM 102 inhibit MM102 TFA Inhibitor inhibitor

 

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