MM-102
For research use only.
Catalog No.S7265 Synonyms: HMTase Inhibitor IX
10 publications
CAS No. 1417329-24-8
MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay.
4 Customer Reviews
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Immunofluorescence staining of H3K4me2/3 (red) in the IVF, SCNT and MM-102-NT embryos. The nuclei (blue) were stained with DAPI. The merged images of H3K4me2/3 and DNA were purple. Scale bars: 50 μm.
Cell Physiol Biochem, 2018, 45(4):1529-1540. MM-102 purchased from Selleck.
(D) ChIP-qPCR analysis of the H3K4me3 levels in hESCs synchronized in mitosis with or without MLL1/2 inhibitors. DMSO, cells treated with DMSO only; Noc, cells blocked in mitosis with nocodazole; Noc + MLL Inh, cells blocked in mitosis with nocodazole in the presence of Mi-2 and MM-102 (20 μM each). Values for percent input are normalized to the IgG control (n = 2). One-way analysis of variance followed by Tukey's test for multiple comparisons was performed. *, P < 10−2; ****, P < 10−5; ns, not significant. (E) Reverse transcription-qPCR analysis of RNA expression levels for bivalent genes after induction of differentiation in unsynchronized H9 ES cells pretreated with MLL inhibitors. Differentiation was induced using E6 medium containing 1 μM RA per 24 h. DMSO, cells pretreated with DMSO only; MLL Inh, cells pretreated with Mi-2 and MM-102 (20 μM each) for 24 h. Unpaired parametric t test with Welch's corrections was performed. Two-tailed P values were calculated. *, P < 10−2; **, P < 10−3; ***, P < 10−4; ns, not significant. Log2 RNA levels were normalized against HPRT1 RNA levels and expressed as fold change between undifferentiated and differentiated cells.
Mol Cell Biol, 2015, 36(4):615-27. MM-102 purchased from Selleck.
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(d-e) The viability of cells treated with cisplatin and MM-102 for 24h in concentrations as indicated was determined CCK-8 assay.
Int J Biol Sci, 2018, 14(9):1122-1132. MM-102 purchased from Selleck.
NHMCs were incubated 24 h in 5.6 (white bars) or 25 mM glucose (black bars) in the presence or absence of TSA (200 nM) or MM-102 (50 μM) as indicated. mRNA was extracted from the cells after incubation and SPP1 expression was quantified by qPCR and normalized to housekeeping genes HPRT and PPIb expression. The values represent the mean ± SEM of five to eleven independent experiments. *p < 0.05, ***p < 0.001 vs. 5.6 mM glucose without inhibitors; yp < 0.05 vs. 25 mM glucose without inhibitors.
Biochem Biophys Res Commun, 2016, 469(1):108-13. MM-102 purchased from Selleck.
Purity & Quality Control
Choose Selective Histone Methyltransferase Inhibitors
Biological Activity
| Description | MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay. | |||||||||||||||||||||||
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| In vitro |
MM-102, as a MLL1 mimetic, shows high binding affinities to WDR5 with IC50 of 2.9 nM and Ki of < 1 nM. In the MLL1-AF9 transduced murine cells, MM-102 specifically reduces expression of two critical MLL1 target genes (HoxA9 and Meis-1), which are required for MLL1 mediated leukemogenesis. In addition, MM-102 effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins. [1] |
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| Assay |
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Protocol
| Kinase Assay: |
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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. |
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| Cell Research: |
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (149.29 mM) |
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| Water | 100 mg/mL (149.29 mM) | |
| Ethanol | '100 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 669.8 |
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| Formula | C35H49F2N7O4 |
| CAS No. | 1417329-24-8 |
| Storage |
powder in solvent |
| Synonyms | HMTase Inhibitor IX |
| Smiles | CCC(CC)(C(=O)NC(CCCN=C(N)N)C(=O)NC1(CCCC1)C(=O)NC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)NC(=O)C(C)C |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
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Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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