NNMT-IN-6 hydrochloride is a selective nicotinamide N-methyltransferase ( NNMT ) inhibitor with an IC50 of 1.41 μM and a K d of 5.55 μM. NNMT-IN-6 hydrochloride exhibits selectivity over PRMT1 and NSD2. NNMT-IN-6 hydrochloride inhibits cancer cell proliferation and reduces cellular N-methylnicotinamide (MNA) production. NNMT-IN-6 hydrochloride can be used for the research of oral cancer [1].
In Vitro, NNMT-IN-6 (compound 78) (10-100 μM; 24-72 h) hydrochloride dose- and time- dependently inhibits HSC-2 human oral cancer cell proliferation[1]. NNMT-IN-6 (100 μM; 0-72 h) hydrochloride inhibits cellular NNMT activity in HSC-2 human oral cancer cells, reducing MNA production by 50% at 100 μM after 48 h[1]. NNMT-IN-6 hydrochloride binds the NNMT active site, forms π-π stacking interactions with tyrosine residues in the nicotinamide binding pocket, and forms an intramolecular hydrogen bond that stabilizes its binding conformation.
References:
[1]. Gao Y, et al. Bisubstrate Inhibitors of Nicotinamide N -Methyltransferase (NNMT) with Enhanced Activity. J Med Chem. 2019;62(14):6597-6614.
In Vitro, NNMT-IN-6 (compound 78) (10-100 μM; 24-72 h) hydrochloride dose- and time- dependently inhibits HSC-2 human oral cancer cell proliferation[1]. NNMT-IN-6 (100 μM; 0-72 h) hydrochloride inhibits cellular NNMT activity in HSC-2 human oral cancer cells, reducing MNA production by 50% at 100 μM after 48 h[1]. NNMT-IN-6 hydrochloride binds the NNMT active site, forms π-π stacking interactions with tyrosine residues in the nicotinamide binding pocket, and forms an intramolecular hydrogen bond that stabilizes its binding conformation.
References:
[1]. Gao Y, et al. Bisubstrate Inhibitors of Nicotinamide N -Methyltransferase (NNMT) with Enhanced Activity. J Med Chem. 2019;62(14):6597-6614.