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  • Bisubstrate Inhibitor 78
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Bisubstrate Inhibitor 78

An inhibitor of NNMT

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Bisubstrate Inhibitor 78的二维码
  • 库存: 现货
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  • 500ug
    ¥2800.00
    2240.00
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  • 1mg
    ¥5275.00
    4220.00
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  • 5mg
    ¥24700.00
    19760.00
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  • 货号: ajcx24094
  • CAS: 2368247-39-4
  • 别名:
  • 分子式: C25H29N7O5
  • 分子量: 507.5
  • 纯度: >98%
  • 溶解度: Chloroform: slightly soluble,DMF: slightly soluble,DMSO: slightly soluble,Ethanol: slightly soluble,Methanol: slightly soluble
  • 储存: -20°C
  • 库存: 现货

Background

Bisubstrate inhibitor 78 is an inhibitor of nicotinamide N-methyltransferase (NNMT; IC50 = 1.41 µM).1 It binds the NNMT active site in the binding pockets for the NNMT substrates S-adenosyl-L-methionine (SAM) and nicotinamide . Bisubstrate inhibitor 78 is selective for NNMT over histone-lysine N-methytransferase NSD2 and protein arginine methyltransferase 1 (PRMT1; IC50s = >50 µM for both). It reduces levels of 1-methylnicotinamide in, and inhibits proliferation of, HSC-2 oral cancer cells when used at a concentration of 100 µM.



1.Gao, Y., van Haren, M.J., Moret, E.E., et al.Bisubstrate inhibitors of nicotinamide N-methyltransferase (NNMT) with enhanced activityJ. Med. Chem.62(14)6597-6614(2019)

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