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I3MT-3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
I3MT-3图片
CAS NO:459420-09-8
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
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=2.7μM)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。
Cas No.459420-09-8
别名HMPSNE
Canonical SMILESO=C1NC(SCC(C2=C3C=CC=CC3=CC=C2)=O)=NC(C)=C1
分子式C17H14N2O2S
分子量310.37
溶解度DMSO: 125 mg/mL (402.75 mM)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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[1].

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[1].I3MT-3 (1 μM) 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 µM[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 µM with a cozncentration-dependent decrease of AzMC fluorescence[1].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)[2].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 rate (OCR) profiles in CT26 cells[2].I3MT-3 (0-300 μM; 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]. Cell Proliferation Assay[2] Cell Line: CT26 cells

[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.