TargetMol

Bisubstrate Inhibitor 78

Product Code:
 
TAR-T36802
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1

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CodeSizePrice
TAR-T36802-5mg5mg£850.00
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TAR-T36802-50mg50mg£1,661.00
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TAR-T36802-100mg100mg£2,079.00
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This product comes from: United States.
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Further Information

Bioactivity:
Bisubstrate inhibitor 78 is an inhibitor of nicotinamide N-methyltransferase (NNMT; IC50= 1.41 μM).1It 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.
CAS:
2368247-39-4
Formula:
C25H29N7O5
Molecular Weight:
507.5
Purity:
0.98
SMILES:
OC([C@@H](N)CCN(CC1=CC(C=CC=C2)=C2C=C1)C[C@@H]3[C@@H](O)[C@@H](O)[C@H](N4C5=NC=NC(N)=C5N=C4)O3)=O

References

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)