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.
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- CAS 番号: 2587612-25-5
- 分子式: C24H32N8O6
- 分子量:528.56
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Histone Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
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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.
化学情報
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CAS 番号 2587612-25-5
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分子量 528.56
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MS2734 関連分類
HY-111367 関連分類
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