I3MT-3

459420-09-8

310.37

10 mM in DMSO

Stem Cell/Wnt

I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC₅₀=2.7 uM). 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]. IC50 & Target: IC50: 2.7 uM (3-Mercaptopyruvate sulfurtransferase (3MST))^[1] In Vitro: I3MT-3 (1?uM) is selective for 3MST and shows a high inhibitory activity (80-90%) even at 10?uM in cell lysate of 3MST-overexpressing HEK293 cells. Besides, it is almost inactive towards the other two H2S-producing enzymes even at 100 uM^[1].
I3MT-3 (1?uM) shows a high selectivity for 3MST, it completely suppresses the 3MST activity in COS7 cells living cells^[1].
I3MT-3 produces a concentration-dependent inhibition of the AzMC (the fluorescent H2S probe) signal when incubated with purified human recombinant enzyme, the inhibition of the catalytic activity of 3-MST produces a concentration-dependent inhibition of H2S production with an IC₅₀ of 13.6 uM^[1].
I3MT-3 shows a dose-dependent inhibition of 3-MST activity from CT26 homogenates, which contain the murine form of the enzyme. The IC₅₀ of HMPSNE for murine 3-MST is calculated as 2.3 uM with a cozncentration-dependent decrease of AzMC fluorescence^[1].
I3MT-3 (10 uM-100 uM; after 3 h probe AzMC) causes a partial inhibition of the signal, while at 100 uM, HMPSNE causes a complete inhibition of the AzMC-guided H2S fluorescence at 100 uM, Additionally, HMPSNE is capable of inhibiting its target in situ in CT26 cells (with an IC₅₀ of approximately 30 uM)^[2].
I3MT-3 (0-300 uM; 5-50 hours) does not enhance MTT conversion at 10 uM, while at 100 and 300 uM it produces an inhibitory response, without increasing the LDH signal, i.e., without inducing any detectable degree of cell necrosis. It also produces a decreased oxygen consumption rate (OCR) profiles in CT26 cells^[2].
I3MT-3 (0-300 uM; 48 hours) inhibits CT26 cells proliferate with increasing concentrations of I3MT-3. Confluence of cells treated with HMPSNE is recorded each hour for 48 h by the IncuCyte method^[2].