MMP2-IN-1
Based on 2 publication(s) in Google Scholar
MMP2-IN-1 is a moderate potenet MMP2 inhibitor with IC50 of 6.8 µM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certain cancer cells by arresting the cell cycle and inducing apoptosis.
For research use only. We do not sell to patients.
- Purity : 99.25%
- CAS No.: 2764598-01-6
- Formula: C15H13NO5S
- Molecular Weight:319.33
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MMP2-IN-1
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Biological Activity
Description
IC50 & Target
[1]|
MMP2 6.8 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.11 μM
Compound: 4a
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Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay
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[PMID: 35255412] |
| HeLa | IC50 |
0.18 μM
Compound: 4a
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Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay
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[PMID: 35255412] |
| HepG2 | IC50 |
>10 μM
Compound: 4a
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Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay
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[PMID: 35255412] |
| MDA-MB-231 | IC50 |
0.07 μM
Compound: 4a
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 74 hrs by SRB assay
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[PMID: 35255412] |
In Vitro
MMP2-IN-1 (compound 4a) (0-10 μM; 74 hours) exhibits IC50 values of 0.07 μM, 0.11 μM, and 0.18 μM against MDA-MB-231, A549, and HeLa cancer cells, respectively, and over 10 μM in Hep 5G cells[1].
MMP2-IN-1 (10 μM; 24 hours) induces cell cycle arrest in the S phase[1].
MMP2-IN-1 (0.01 μM, 0.1 μM, 1 μM and 10 μM; 24 hours) induces a dose-dependent increment in early-and late-stage apoptosis of MDA-MB-231 cells, and increased the early-stage apoptosis percentage from 4.66% to 10.9% at 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MDA-MB-231, A549, HeLa and Hep 5G cells[1]
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Concentration:0-10 μM
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Incubation Time:74 hours
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Result:Exhibited IC50 values of 0.07 μM, 0.11 μM, and 0.18 μM against MDA-MB-231, A549, and HeLa cancer cells, respectively, and over 10 μM in Hep 5G cells.
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Cell Line:MDA-MB-231[1]
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Concentration:10 μM
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Incubation Time:24 hours
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Result:Induced cell cycle arrest in the S phase.
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Cell Line:MDA-MB-231[1]
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Concentration:0.01 μM, 0.1 μM, 1 μM and 10 μM
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Incubation Time:24 hours
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Result:Induced a dose-dependent increment in early-and late-stage apoptosis of MDA-MB-231 cells, and increased the early-stage apoptosis percentage from 4.66% to 10.9% at 10 μM.
In Vivo
MMP2-IN-1 (10 mg/kg; IP, daily, for 14 days) significantly inhibits tumor growth in metastatic 4T1 murine breast cancer model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming mice (n = 10, half male and half female)[1]
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Dosage:100 mg/kg, 150 mg/kg, 200 mg/kg, 250 mg/kg
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Administration:IP, single
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Result:No mortality occurred after administration of 100 mg/kg, and the mortality rate was 30%, 50% and 60% at dosing 150 mg/kg, 200 mg/kg, 250 mg/kg respectively.
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Animal Model:Orthotopic 4T1 tumor-bearing mice[1]
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Dosage:10 mg/kg
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Administration:IP, daily, for 14 days
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Result:Significantly inhibited tumor growth in metastatic 4T1 murine breast cancer model.
Chemical Information
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CAS No. 2764598-01-6
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Appearance Solid
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Molecular Weight 319.33
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Formula C15H13NO5S
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Color White to off-white
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SMILES
O=C1COC2(C=CC(C=C2)=O)N1S(=O)(C3=CC=C(C)C=C3)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (313.16 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)
In Vivo:
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 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (7.83 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.83 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 3.1316 mL | 15.6578 mL | 31.3156 mL | 78.2889 mL |
| 5 mM | 0.6263 mL | 3.1316 mL | 6.2631 mL | 15.6578 mL | |
| 10 mM | 0.3132 mL | 1.5658 mL | 3.1316 mL | 7.8289 mL | |
| 15 mM | 0.2088 mL | 1.0439 mL | 2.0877 mL | 5.2193 mL | |
| 20 mM | 0.1566 mL | 0.7829 mL | 1.5658 mL | 3.9144 mL | |
| 25 mM | 0.1253 mL | 0.6263 mL | 1.2526 mL | 3.1316 mL | |
| 30 mM | 0.1044 mL | 0.5219 mL | 1.0439 mL | 2.6096 mL | |
| 40 mM | 0.0783 mL | 0.3914 mL | 0.7829 mL | 1.9572 mL | |
| 50 mM | 0.0626 mL | 0.3132 mL | 0.6263 mL | 1.5658 mL | |
| 60 mM | 0.0522 mL | 0.2610 mL | 0.5219 mL | 1.3048 mL | |
| 80 mM | 0.0391 mL | 0.1957 mL | 0.3914 mL | 0.9786 mL | |
| 100 mM | 0.0313 mL | 0.1566 mL | 0.3132 mL | 0.7829 mL |
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