4(3H)-Pyrimidinone, 6-methyl-2-[[2-(1-naphthalenyl)-2-oxoethyl]thio]-

Uses

I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes.I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST[1].

Biological Activity

I3MT-3 (HMPSNE) is a potent, selective and cell membrane permeable inhibitor of 3-mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM), inactive against other hydrogen sulfide/sulfanilamide sulfur enzymes. I3MT-3 targets a perthiocysteine residue located in the active site of 3MST.

target

References

[1] Kenjiro Hanaoka, et al. Discovery and Mechanistic Characterization of Selective Inhibitors of H 2 S-producing Enzyme: 3-Mercaptopyruvate Sulfurtransferase (3MST) Targeting Active-site Cysteine Persulfide. Sci Rep. 2017 Jan 12;7:40227 DOI:10.1038/srep40227
[2] Fiona Augsburger, et al. Role of 3-Mercaptopyruvate Sulfurtransferase in the Regulation of Proliferation, Migration, and Bioenergetics in Murine Colon Cancer Cells. Biomolecules. 2020 Mar 13;10(3):447. DOI:10.3390/biom10030447