GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.
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.This compound is unstable in powder form and other related salt forms are recommended.
SAHO is a sulfoxide form of the methyl donor S-(5'-adenosyl)-L-methionine chloride and a substrate for radical SAM enzymes.1It is reductively cleaved to S-adenosylhomocysteine , 5'-deoxyadenosine , and 5'-thioadenosine sulfenic acid by the radical SAM enzymes NosL or NosN. 1.Mandalapu, D., Ji, X., and Zhang, Q.Reductive cleavage of sulfoxide and sulfone by two radical S-adenosyl-L-methionine enzymesBiochemistry58(1)36-39(2019)
SAHO2is a sulfone form of the methyl donor S-(5'-adenosyl)-L-methionine chloride and is a substrate for radical SAM enzymes.1It is reductively cleaved to 5'-deoxyadenosine and 5'-thioadenosine sulfinic acid by the radical SAM enzymes NosL or NosN. 1.Mandalapu, D., Ji, X., and Zhang, Q.Reductive cleavage of sulfoxide and sulfone by two radical S-adenosyl-L-methionine enzymesBiochemistry58(1)36-39(2019)
5'-chloro-5'-Deoxyadenosine (hydrate) is a nucleoside analog used as a substrate in polyketide biosynthesis. S-(5'-adenosyl)-L-methionine can be converted to 5'-chloro-5'-deoxyadenosine in a reaction catalyzed by a SAM-dependent chlorinase. Through a 7-step route, 5'-chloro-5'-deoxyadenosine can be converted to chloroethylmalonyl-CoA, which has been shown to be involved in the biosynthesis of the anticancer agent salinosporamide A in the marine bacterium S. tropica.