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Purity: ≥98%
I3MT-3 (also known as HMPSNE; EMT inhibitor-1; EMT inhibitor 1) is a novel, selective, potent, and membrane permeable inhibitor of 3MST (3-Mercaptopyruvate sulfurtransferase) with IC50 of 2.7 μM.
| ln Vitro |
Even at 10 μM, I3MT-3 (1 μM) has strong inhibitory activity (80–90%) in the interstitium of HEK293 cells overexpressing 3MST. It is selective for 3MST. Furthermore, even at 100 μM, it has strong inhibitory action (80–90%). In live COS7 cells, I3MT-3 (1 μM) totally inhibits 3MST activity and shows significant alkalinity towards 3MST [1]. I3MT-3 reduces the concentration oscillation of the AzMC (fluorescent H2S label) signal when buffered with blocked human recombinase. It also inhibits the catalytic activity of 3-MST to inhibit the concentration oscillation of H2S generation. The dosage suppression of 3-MST activity from CT26 balanced slurry, which contains the murine form of the enzyme, is shown in I3MT-Figure 3 with an IC50 of 13.6 μM [1]. 2.3 μM was determined to be the IC50 of HMPSNE against mouse 3-MST, and AzMC fluorescence decreased with concentration inhibition [. A minor reduction of the signal was observed with I3MT-3 (10 μM-100 μM; AzMC after 3 hours of detection), however at 100 μM, HMPSNE entirely blocked AzMC-guided H2S fluorescence. Furthermore, HMPSNE shown the ability to inhibit its target, which is present in CT26 cells in situ (IC50 = 30 μM) [2]. I3MT-3 (0-300 μM; 5-50 hours) generates an inhibitory response without enhancing LDH signaling at 100 and 300 μM, meaning that cells do not trigger any discernible degree of apoptosis. However, it does not increase MTT turnover at 10 μM. The CT26 oxygen consumption rate (OCR) curve will be lowered as a result [2]. As I3MT-3 concentration rises (from 0-300 μM; 48 hours), CT26 cell growth is inhibited. Using the IncuCyte method, the confluency of HMPSNE-treated cells over a 48-hour period was meticulously observed [2].
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| Cell Assay |
Cell proliferation analysis [2]
Cell Types: CT26 cells Tested Concentrations: 0 μM; 10 μM; 30 μM; 100 μM; 300 μM Incubation Duration: 48 hrs (hours) Experimental Results: Slowed down the proliferation of CT26 cells. |
| References |
[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. |
| Molecular Formula |
C₁₇H₁₄N₂O₂S
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|---|---|
| Molecular Weight |
310.37
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| CAS # |
459420-09-8
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| SMILES |
S(C1=NC(C)=CC(N1)=O)CC(C1=CC=CC2C=CC=CC1=2)=O
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| Synonyms |
HMPSNE EMT inhibitor-1EMT inhibitor 1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~402.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (6.70 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2220 mL | 16.1098 mL | 32.2196 mL | |
| 5 mM | 0.6444 mL | 3.2220 mL | 6.4439 mL | |
| 10 mM | 0.3222 mL | 1.6110 mL | 3.2220 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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