MS2734
MS2734 is a dual-substrate NNMT inhibitor that acts as a SAM (HY-B0617) competitor and a non-competitor of Nicotinamide (HY-B0150), with an IC50 of 14 μM and a Kd of 2.7 μM against hNNMT. MS2734 inhibits the methyltransferase activities of DOT1L (IC50 1.3 μM), PRMT7 (IC50 20 μM), BCDIN3D (IC50 40 μM) and SMYD2 (IC50 62 μM). MS2734 is applicable to research related to diabetes, obesity and various cancers.
For research use only. We do not sell to patients.
- CAS No.: 2587612-25-5
- Formula: C24H32N8O6
- Molecular Weight:528.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
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NNMT 14 μM (IC50) |
DOT1L 1.3 μM (IC50) |
PRMT7 20 μM (IC50) |
SMYD2 62 μM (IC50) |
BCDIN3D 40 μM (IC50) |
MS2734 (250 nM-250 μM) inhibits the methyltransferase activity of purified hNNMT in the SAHH-coupled fluorescence assay, with an IC50 of 14 μM[1].
MS2734 binds directly to purified hNNMT, with a Kd value of 2.7 μM measured by ITC[1].
MS2734 exhibits better selectivity for hNNMT than most tested methyltransferases and acetyltransferases, and shows significant inhibitory effects on DOT1L (IC50 = 1.3 μM), PRMT7 (IC50 = 20 μM), BCDIN3D (IC50 = 40 μM) and SMYD2 (IC50 = 62 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2587612-25-5
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Molecular Weight 528.56
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Formula C24H32N8O6
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SMILES
O[C@@H]1[C@H](O)[C@@H](CN(CCC[C@H](N)C(O)=O)CCC2=CC(C(N)=O)=CC=C2)O[C@H]1N3C=NC4=C(N)N=CN=C43
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Babault N, et al. Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT). J Med Chem. 2018 Feb 22;61(4):1541-1551. doi: 10.1021/acs.jmedchem.7b01422. Epub 2018 Jan 31. Erratum in: J Med Chem. 2018 Jul 12;61(13):5771-5772. [Content Brief]
[2]. Policarpo RL, et al. High-Affinity Alkynyl Bisubstrate Inhibitors of Nicotinamide -Methyltransferase (NNMT). Journal of medicinal chemistry. 2019 Nov 14;62(21):9837-9873. [Content Brief]
[3]. Li XY, et al. Nicotinamide N-Methyltransferase: A Promising Biomarker and Target for Human Cancer Therapy. Frontiers in oncology. 2022;12:894744. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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