I3MT-3 (HMPSNE) 是有效、选择性和具有细胞膜渗透性的 3-巯基丙酮酸硫转移酶 (3MST) (IC₅₀=2.7 μM) 的抑制剂，对其他硫化氢/磺胺制硫酶没有活性。I3MT-3 靶向位于 3MST 活性位点的过硫半胱氨酸残基。

I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC 50 =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.

Solid

IC50: 2.7 μM (3-Mercaptopyruvate sulfurtransferase (3MST))

I3MT-3 (1?μM) is selective for 3MST and shows a high inhibitory activity (80–90%) even at 10?μM in cell lysate of 3MST-overexpressing HEK293 cells. Besides, it is almost inactive towards the other two H2S-producing enzymes even at 100 μM.
I3MT-3 (1?μM) shows a high selectivity for 3MST, it completely suppresses the 3MST activity in COS7 cells living cells.
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 μM.
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 μM with a coznc

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Powder -20°C 3 years；In solvent -80°C 6 months

[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
[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.

In Vitro: DMSO : 125 mg/mL (402.75 mM; Need ultrasonic)配制储备液