I3MT-3
Based on 5 publication(s) in Google Scholar
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.
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- Pureza: 99.76%
- No. CAS: 459420-09-8
- Fòrmula: C17H14N2O2S
- Peso molecular:310.37
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) I3MT-3
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Cell Proliferation/Viability Assay
Actividad biológica
IC50: 2.7 μM (3-Mercaptopyruvate sulfurtransferase (3MST))[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CT26 | IC50 |
207 μM
Compound: 1a
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Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell proliferation measured after 48 hrs by IncuCyte live-cell imaging assay
Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell proliferation measured after 48 hrs by IncuCyte live-cell imaging assay
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[PMID: 33856792] |
| CT26 | IC50 |
243 μM
Compound: 1a
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Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
Antiproliferative activity against mouse CT26 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
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[PMID: 33856792] |
| MC-38 | IC50 |
101 μM
Compound: 1a
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Antiproliferative activity against mouse MC38 cells assessed as inhibition of cell proliferation measured after 48 hrs by IncuCyte live-cell imaging assay
Antiproliferative activity against mouse MC38 cells assessed as inhibition of cell proliferation measured after 48 hrs by IncuCyte live-cell imaging assay
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[PMID: 33856792] |
| MC-38 | IC50 |
221 μM
Compound: 1a
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Antiproliferative activity against mouse MC38 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
Antiproliferative activity against mouse MC38 cells assessed as inhibition of cell proliferation measured after 24 hrs by MTT assay
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[PMID: 33856792] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CT26 cells
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Concentration:0 μM; 10 μM; 30 μM; 100 μM; 300 μM
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Incubation Time:48 hours
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Result:Slowed down proliferation of CT26 cells.
Chemical Information
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No. CAS 459420-09-8
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Appearance Solid
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Peso molecular 310.37
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Fòrmula C17H14N2O2S
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Color Off-white to light brown
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SMILES
O=C1NC(SCC(C2=C3C=CC=CC3=CC=C2)=O)=NC(C)=C1
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Synonyms
HMPSNE
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
Glioblastoma cell motility depends on enhanced oxidative stress coupled with mobilization of a sulfurtransferase. [Abstract]2022 Oct 30;13(10):913. PMID: 36310164
I3MT-3 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Oct 30;13(10):913. [Abstract]
Mann-Whitney test. Inhibiting MPST enzymatic activity using the pharmacological inhibitor I3-MT-3 decreases cell migration on Matrigel. Cells treated with 200 µM I3-MT-3 or vehicle for 72 h (R633, P3) or 45 h (GBO). Migration assessed 48 h (R633, P3) and 45 h (GBO) post-seeding.
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Int J Mol Sci
2025 Mar 2;26(5):2237. PMID: 40076859 -
Biochim Biophys Acta Mol Basis Dis
BRD9 status is a major contributor for cysteine metabolic remodeling through MST and EAAT3 modulation in malignant melanoma. [Abstract]2024 Feb;1870(2):166983. PMID: 38070581 -
J Biol Chem
Reactive sulfur species disaggregate the SQSTM1/p62-based aggresome-like induced structures via the HSP70 induction and prevent parthanatos. [Abstract]2023 Jun;299(6):104710. PMID: 37060999 -
Solvente y solubilidad
DMSO : 125 mg/mL (402.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (6.70 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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 [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2220 mL | 16.1098 mL | 32.2196 mL | 80.5490 mL |
| 5 mM | 0.6444 mL | 3.2220 mL | 6.4439 mL | 16.1098 mL | |
| 10 mM | 0.3222 mL | 1.6110 mL | 3.2220 mL | 8.0549 mL | |
| 15 mM | 0.2148 mL | 1.0740 mL | 2.1480 mL | 5.3699 mL | |
| 20 mM | 0.1611 mL | 0.8055 mL | 1.6110 mL | 4.0275 mL | |
| 25 mM | 0.1289 mL | 0.6444 mL | 1.2888 mL | 3.2220 mL | |
| 30 mM | 0.1074 mL | 0.5370 mL | 1.0740 mL | 2.6850 mL | |
| 40 mM | 0.0805 mL | 0.4027 mL | 0.8055 mL | 2.0137 mL | |
| 50 mM | 0.0644 mL | 0.3222 mL | 0.6444 mL | 1.6110 mL | |
| 60 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3425 mL | |
| 80 mM | 0.0403 mL | 0.2014 mL | 0.4027 mL | 1.0069 mL | |
| 100 mM | 0.0322 mL | 0.1611 mL | 0.3222 mL | 0.8055 mL |
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