MM-102
Based on 4 publication(s) in Google Scholar
MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos.
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- Pureza: 99.09%
- No. CAS: 1417329-24-8
- Fòrmula: C35H49F2N7O4
- Peso molecular:669.80
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Almacenamiento:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MM-102
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
37.8 μM
Compound: MM-102
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Growth inhibition of human K562 cells after 7 days by MTS assay
Growth inhibition of human K562 cells after 7 days by MTS assay
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[PMID: 27598236] |
| K562 | IC50 |
37.8 μM
Compound: MM-102
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Antiproliferative activity against human K562 cells harboring BCR-ABL assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay
Antiproliferative activity against human K562 cells harboring BCR-ABL assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay
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[PMID: 27720555] |
| MV4-11 | IC50 |
20.7 μM
Compound: MM-102
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Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein after 72 hrs by CCK8 assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein after 72 hrs by CCK8 assay
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[PMID: 27598236] |
| MV4-11 | IC50 |
20.7 μM
Compound: MM-102
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Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay
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[PMID: 27720555] |
| MV4-11 | IC50 |
25 μM
Compound: MM-102
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Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein by CellTiter-Glo assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein by CellTiter-Glo assay
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[PMID: 27598236] |
| MV4-11 | IC50 |
25 μM
Compound: MM-102
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Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 after 7 days by CellTiter-Glo luminescent cell viability Assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 after 7 days by CellTiter-Glo luminescent cell viability Assay
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[PMID: 27720555] |
MM-102 (40 µM; 4 d) induces growth arrest and cell death in MLL1-AF9-transformed mouse leukemia cells specifically in leukemia cells harboring the MLL1 translocation, but does not interfere with the growth of normal bone marrow[2]. MM-102 (2, 10, and 50 µM) disrupts the association of WDR5 and RbBP5 with GSTMLL1 in a concentration-dependent manner. The association of WDR5 with MLL1 is mildly disrupted at 2 µM, moderately disrupts at 10 µM, and completely disrupts at 50 µM[2]. MM-102 specifically inhibits the methyltransferase activity of the MLL1 complex with an IC50 value of 0.32 µM[2]. MM-102 (50 µM; 48 h) can significantly inhibit the proliferation, migration and chemoresistance of TFK1 and RBE cells[3]. MM-102 (50 µM; 1 h) not only significantly reduces the expression of MLL1, WDR5 and H3K4me3 in TGF-b1-stimulated NRK-49F cells, but also inhibits the expression of p16INK4a[4]. MM-102 (50-100 μM; 48 h) enhances the developmental competence of porcine SCNT embryos and improves the expression pattern of key genes in SCNT embryo development[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TFK1 and RBE cells
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Concentration:50 µM
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Incubation Time:48 h
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Result:Inhibited the expression of ABCB1, but had no effect on the expression of MBD2 and WDR5.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ischemia-reperfusion injury in mice[4]
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Dosage:15 mg/kg
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Administration:i.p.; Once daily for 7 days
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Result:Inhibited a-SMA protein expression.
Inhibited p-NF-kB (p65), IL-1b, TNF-a, and IL-6 mRNA expression.
Chemical Information
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No. CAS 1417329-24-8
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Appearance Solid
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Peso molecular 669.80
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Fòrmula C35H49F2N7O4
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Color White to off-white
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SMILES
O=C(C1(NC([C@@H](NC(C(NC(C(C)C)=O)(CC)CC)=O)CCCNC(N)=N)=O)CCCC1)NC(C2=CC=C(F)C=C2)C3=CC=C(F)C=C3
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Synonyms
HMTase Inhibitor IX
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
Histone methyltransferase MLL1 drives renal tubular cell apoptosis by p53-dependent repression of E-cadherin during cisplatin-induced acute kidney injury. [Abstract]2022 Sep 6;13(9):770. PMID: 36068197 -
Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431 -
J Mol Endocrinol
2021 Jan;66(1):45-57. PMID: 33151904
Solvente y solubilidad
DMSO : 125 mg/mL (186.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Karatas H, et al. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. J Am Chem Soc. 2013, 135(2), 669-682. [Content Brief]
[3]. Wang D, et al. MBD2 regulates the progression and chemoresistance of cholangiocarcinoma through interaction with WDR5[J]. Journal of Experimental & Clinical Cancer Research, 2024, 43(1): 272. [Content Brief]
[4]. Hara D, et al. Inhibition of H3K4 Trimethylation Ameliorates Peritoneal Fibrosis and Senescence: FR-PO456[J]. Journal of the American Society of Nephrology, 2022, 33(11S): 447-448. [Content Brief]
[5]. Zhang Z, et al. Down-regulation of H3K4me3 by MM-102 facilitates epigenetic reprogramming of porcine somatic cell nuclear transfer embryos[J]. Cellular Physiology and Biochemistry, 2018, 45(4): 1529-1540. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4930 mL | 7.4649 mL | 14.9298 mL | 37.3246 mL |
| 5 mM | 0.2986 mL | 1.4930 mL | 2.9860 mL | 7.4649 mL | |
| 10 mM | 0.1493 mL | 0.7465 mL | 1.4930 mL | 3.7325 mL | |
| 15 mM | 0.0995 mL | 0.4977 mL | 0.9953 mL | 2.4883 mL | |
| 20 mM | 0.0746 mL | 0.3732 mL | 0.7465 mL | 1.8662 mL | |
| 25 mM | 0.0597 mL | 0.2986 mL | 0.5972 mL | 1.4930 mL | |
| 30 mM | 0.0498 mL | 0.2488 mL | 0.4977 mL | 1.2442 mL | |
| 40 mM | 0.0373 mL | 0.1866 mL | 0.3732 mL | 0.9331 mL | |
| 50 mM | 0.0299 mL | 0.1493 mL | 0.2986 mL | 0.7465 mL | |
| 60 mM | 0.0249 mL | 0.1244 mL | 0.2488 mL | 0.6221 mL | |
| 80 mM | 0.0187 mL | 0.0933 mL | 0.1866 mL | 0.4666 mL | |
| 100 mM | 0.0149 mL | 0.0746 mL | 0.1493 mL | 0.3732 mL |
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