產(chǎn)品描述: | 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 |
靶點: |
IC50: 2.7 μM (3-Mercaptopyruvate sulfurtransferase (3MST));Hippopathway |
體外研究: |
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 cozncentration-dependent decrease of AzMC fluorescence.
I3MT-3 (10 μM-100 μM; after 3 h probe AzMC) causes a partial inhibition of the signal, while at 100 μM, HMPSNE causes a complete inhibition of the AzMC-guided H2S fluorescence at 100 μM, Additionally, HMPSNE is capable of inhibiting its target in situ in CT26 cells (with an IC50 of approximately 30 μM).
I3MT-3 (0-300 μM; 5-50 hours) does not enhance MTT conversion at 10 μM, while at 100 and 300 μM 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 rat |
參考文獻: |
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. |
溶解性: |
Soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
3.222 ml |
16.11 ml |
32.22 ml |
5 mM |
0.644 ml |
3.222 ml |
6.444 ml |
10 mM |
0.322 ml |
1.611 ml |
3.222 ml |
50 mM |
0.064 ml |
0.322 ml |
0.644 ml |
|
注意: |
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