Art. -Nr.: HY-12169

Marimastat

Name: Marimastat
Brand: MedChemExpress
SKU: HY-12169
Price: 68.00 USD
Availability: InStock
Rating: 5 (22 reviews)

(Synonyms: BB2516; TA2516)

22 Cited Publications

Kundenbewertung

Based on 22 publication(s) in Google Scholar

Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs, with potent activity against MMP-9 (IC₅₀=3 nM), MMP-1 (IC₅₀=5 nM), MMP-2 (IC₅₀=6 nM), MMP-14 (IC₅₀=9 nM) and MMP-7 (IC₅₀=13 nM), used in the treatment of cancer. Marimastat (BB2516) is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes.

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Reinheit : 99.90%
CAS. Nr.: 154039-60-8
Formel: C₁₅H₂₉N₃O₅
Molecular Weight:331.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Marimastat Chemical Structure

CAS. Nr.: 154039-60-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (22)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (8)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

MMP-3

3 nM (IC₅₀)

MMP-1

5 nM (IC₅₀)

MMP-2

6 nM (IC₅₀)

MMP-14

9 nM (IC₅₀)

MMP-7

13 nM (IC₅₀)

Alle MMP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
THP-1	IC₅₀	2100 nM Compound: 1Marimastat	Selective inhibition of the cellular TNF alpha release from LPS-stimulated THP-1 cells Selective inhibition of the cellular TNF alpha release from LPS-stimulated THP-1 cells	[PMID: 11754593]

In Vitro

Marimastat (BB2516) (1 μM) shows inhibition of vascular outgrowth, and selectively affects angiogenesis^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

Animals receiving chemoradiation + Marimastat (BB2516) (8.7 mg/kg) have statistically significant delayed growth, compared to animals receiving chemoradiation alone. Marimastat (BB2516) may work in combination with chemotherapy and radiation to inhibit tumor growth^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 154039-60-8
Appearance Solid
Molecular Weight 331.41
Formel C₁₅H₂₉N₃O₅
Color White to gray
SMILES

O=C(NO)[C@@H](O)[C@@H](CC(C)C)C(N[C@H](C(NC)=O)C(C)(C)C)=O
Synonyms

BB2516; TA2516
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (22)

All Bio/Physico-chemical AssayWB2D/3D Cell Culture and DifferentiationHistological Imaging/Staining

Sort by:

Journal Impact Factor

Cell Res

s-HBEGF/SIRT1 circuit-dictated crosstalk between vascular endothelial cells and keratinocytes mediates sorafenib-induced hand-foot skin reaction that can be reversed by nicotinamide. [Abstract]

2020 Sep;30(9):779-793. PMID: 32296111

Marimastat purchased from MedChemExpress. Usage Cited in: Cell Res. 2020 Sep;30(9):779-793. [Abstract]

HUVECs were treated with or without sorafenib or marimastat (1 μM) for 24 h. The level of s-HBEGF in the supernatant or pro-HBEGF in total cell lysates was detected by western blot.
Adv Mater

Spatiotemporally Engineered Protein Delivery via Integrated Covalent Coupling and Pathological Triggers for Precision Microenvironment Reprogramming in Tissue Injury Repair. [Abstract]

2025 Sep 22:e12554. PMID: 40981608
Sci Adv

An enzymatic cleavage-triggered minimally invasive nanosensor for urine-based detection of early atherosclerosis. [Abstract]

2025 Mar 14;11(11):eadu7614. PMID: 40085714

Marimastat purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Mar 14;11(11):eadu7614. [Abstract]

Fluorescence analysis of supernatant from foam cells treated with lipopolysaccharide and oxidized low-density lipoprotein, with or without Marimastat (10 μM), followed by incubation with the substrate peptide.
Mol Ther

2016 Dec;24(12):2090-2099. PMID: 28132714
Cell Prolif

LL-37 Inhibits TMPRSS2-Mediated S2' Site Cleavage and SARS-CoV-2 Infection but Not Omicron Variants. [Abstract]

2025 Dec;58(12):e70060. PMID: 40375579

Marimastat purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2025 Dec;58(12):e70060. [Abstract]

293T‐A2 cells were pretreated for 2 h with indicated concentrations of marimastat (0-10 μM), and then SARS‐CoV‐2 spike pseudoparticles pretreated for 2 h with 10 μg/mL of LL‐37 were added to cells. Infection rates were assessed at 2 days post infection by measuring the RLU of luciferase activity.
EMBO Rep

Sensing of mycobacterial arabinogalactan by galectin-9 exacerbates mycobacterial infection. [Abstract]

2021 Jul 5;22(7):e51678. PMID: 33987949

Marimastat purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2021 Jul 5;22(7):e51678. [Abstract]

C57BL/6 mice were left untreated (NT) or were intraperitoneally treated with indicated amounts of AG for 3 days in the absence or presence of the MMP inhibitor marimastat (10 mg/kg) given intraperitoneally prior to AG stimulation. Lung sections stained with H&E and quantification of lung lesion burden from H&E‐stained sections .
Int J Mol Sci

Epithelial PCSK6 Promotes Proliferation and Decreases Collagen Deposition by Fibroblasts Potentially via MMP Activation. [Abstract]

2026 Jun 4;27(11):5104. PMID: 42278627
J Cell Mol Med

Inactivation of CDK12 Enhances Mitochondrial Efficiency to Suppress DNA Damage. [Abstract]

2026 Apr;30(7):e71101. PMID: 41896195
Rheumatology (Oxford)

Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]

2025 Aug 13:keaf437. PMID: 40802538
Bioconjug Chem

Matrix Metalloproteinase Responsive Nanoparticles for Synergistic Treatment of Colorectal Cancer via Simultaneous Anti-Angiogenesis and Chemotherapy. [Abstract]

2016 Dec 21;27(12):2943-2953. PMID: 27998073

Marimastat purchased from MedChemExpress. Usage Cited in: Bioconjug Chem. 2016 Dec 21;27(12):2943-2953. [Abstract]

Accumulative release of CPT from nanoparticles in different media: PBS buffer with MMP-2, PBS buffer, PBS buffer with MMP-2 and MMP-2 inhibitor Marimastat (1 mM).

Marimastat purchased from MedChemExpress. Usage Cited in: Bioconjug Chem. 2016 Dec 21;27(12):2943-2953. [Abstract]

Marimastat (1 μM). Representative photos of tumor spheroids after treatment with various formulations and blank controls, the scale bar is 100 μm.

Marimastat purchased from MedChemExpress. Usage Cited in: Bioconjug Chem. 2016 Dec 21;27(12):2943-2953. [Abstract]

Marimastat (1 μM). The ratio of volume change of HT-29 spheres volume (%) after applying different formulations. Data are represented as average ± standard error (n = 3).
Biomed Mater

3-Layer lung cancer invasion model for evaluating MMP-targeted anti-metastatic therapeutics. [Abstract]

2026 Jun 26. PMID: 42361847
Biochim Biophys Acta Mol Cell Biol Lipids

OTUD7B controls oxLDL uptake by stabilizing Lox-1 in THP-1 and U937 cells. [Abstract]

2025 Jun;1870(5):159618. PMID: 40294697
Viruses

Metalloprotease-Dependent S2'-Activation Promotes Cell-Cell Fusion and Syncytiation of SARS-CoV-2. [Abstract]

2022 Sep 21;14(10):2094. PMID: 36298651
Endocrine

125I-Angiotensin 1-7 binds to a different site than angiotensin 1-7 in tissue membrane preparations. [Abstract]

2021 May;72(2):529-538. PMID: 33415576
Biol Reprod

2026 Jul 9:ioag141. PMID: 42424391
PLoS One

Discovery of novel TACE inhibitors using graph convolutional network, molecular docking, molecular dynamics simulation, and Biological evaluation. [Abstract]

2024 Dec 27;19(12):e0315245. PMID: 39729480
Eur Biophys J

A standard operating procedure for an enzymatic activity inhibition assay. [Abstract]

2021 May;50(3-4):345-352. PMID: 33864100
bioRxiv

Multimodal profiling of proinflammatory protease activity identifies caspase-1 as a target for lung cancer interception. [Abstract]

2025 Jul 2:2025.07.01.662195. PMID: 40631193
KTH Royal Institute of Technology

2025.
SSRN

2020 Oct 5.
ACS Comb Sci

Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]

2019 Dec 9;21(12):805-816. PMID: 31689077
Chinese Journal of Biochemical and Pharmaceutics

2017,37(12):1-04.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (301.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0174 mL

15.0871 mL

30.1741 mL

5 mM

0.6035 mL

3.0174 mL

6.0348 mL

10 mM

0.3017 mL

1.5087 mL

3.0174 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

All Signal Pathway Related Cell Biology Histomorphology Animals and Diseases

Mitochondrial membrane-potential fluorescent assay
Mitochondrial membrane potential fluorescent assays estimate ΔΨm in living cells using lipophilic cationic dyes such as TMRM, TMRE, rhodamine 123, and JC-1, which accumulate in mitochondria according to membrane polarization; loss of signal after FCCP or CCCP treatment is interpreted as mitochondrial depolarization. TMRM/TMRE and rhodamine 123 are commonly used for semi-quantitative live-cell microscopy or flow cytometry, while JC-1 can report a shift from red aggregate fluorescence to green monomer fluorescence during depolarization; interpretation requires controls because dye concentration, quenching mode, cell type, dye efflux, and mitochondrial mass can affect fluorescence independently of ΔΨm.
Human pluripotent stem cell endothelial-cell differentiation
Human pluripotent stem cell endothelial differentiation is based on stepwise developmental patterning: early activation of WNT/GSK3β inhibition promotes mesodermal or vascular progenitor entry, followed by endothelial specification using VEGF-related signaling, BMP4, FGF2, Notch modulation, or cAMP depending on the published protocol. Endothelial differentiation is read out by acquisition of CD31, CD34, VE-cadherin/CD144, KDR/VEGFR2, vWF, Tie2, NOS3, acetylated LDL uptake, tube/network formation, barrier function, and in vivo vessel-forming capacity where tested.
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.
Vascular/Branching Fractal Analysis
Vascular/branching fractal analysis quantifies the geometric complexity of vessel trees or vascular networks from segmented 2D images, commonly by converting vessels into binary and/or skeletonized maps and estimating fractal dimension using box-counting or related approaches. Fractal dimension is interpreted as an image-derived readout of vascular branching complexity, space filling, or density, and has been applied to retinal photographs, fluorescein angiography, OCT angiography, capillary perfusion maps, and in vitro Matrigel angiogenesis networks. The assay readout is generated from vessel-positive pixels after image preprocessing, vessel segmentation, binarization, and optional skeletonization; reported outputs include fractal dimension, vessel density, branchpoint density, endpoint density, vessel length density, tortuosity, and generation-based branching metrics when VESGEN-style analysis is used. The biological interpretation is limited to quantitative vascular patterning and s
Mitochondrial membrane-potential and mitochondrial mass staining
Mitochondrial membrane potential staining measures the electrochemical polarization across the mitochondrial inner membrane in live cells using lipophilic cationic fluorescent probes; early rhodamine-based work showed that selective mitochondrial dye accumulation is lost when the mitochondrial transmembrane potential is dissipated. JC-1 reports mitochondrial polarization by shifting from green monomer fluorescence to red J-aggregate fluorescence as dye concentration increases within energized mitochondria; therefore, the red/green fluorescence ratio is used as a relative readout of mitochondrial membrane potential. TMRE or TMRM staining provides a single-channel relative readout because these cationic rhodamine esters accumulate in polarized mitochondria, and lower fluorescence indicates reduced mitochondrial polarization when acquisition and dye-loading conditions are controlled. Mitochondrial mass staining is commonly performed with MitoTracker Green FM or related MitoTracker dyes as
Endothelial Tube Formation Assay
Endothelial tube formation assay evaluates the ability of endothelial cells to attach, migrate, align, and organize into capillary-like networks when cultured on gelled basement membrane extract or Matrigel; the readout is the morphology and quantity of tube-like networks, which reflects an in vitro endothelial morphogenesis step related to angiogenesis. Basement membrane extract/Matrigel provides laminin-rich extracellular matrix cues that support endothelial differentiation into capillary-like structures, but it can contain biologically active growth factors, so growth-factor-reduced matrix is preferred when testing defined angiogenic stimulators or inhibitors.
Endothelial Cell Migration/Angiogenic Sprouting Assay
Endothelial cell migration and angiogenic sprouting assays are in vitro (and partially ex vivo-adapted) functional models that quantify the ability of endothelial cells to undergo coordinated migration, extracellular matrix invasion, and multicellular organization into capillary-like sprouts in response to pro-angiogenic stimuli such as VEGF, bFGF, or conditioned microenvironments. These assays are used to model early angiogenic events including tip-cell formation, directional migration, and lumen-like sprout extension, which collectively reflect angiogenic activation and vascular morphogenesis processes observed in vivo.
Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Rasmussen HS, et al. Matrix metalloproteinase inhibition as a novel anticancer strategy: a review with special focus on batimastat and marimastat. Pharmacol Ther. 1997;75(1):69-75. [Content Brief]

[2]. Yu M, et al. Incorporation of Bulky and Cationic Cyclam-Triazole Moieties into Marimastat Can Generate Potent MMP Inhibitory Activity without Inducing Cytotoxicity. ChemistryOpen. 2013 Jun;2(3):99-105. [Content Brief]

[3]. van Wijngaarden J, et al. An in vitro model that can distinguish between effects on angiogenesis and on established vasculature: actions of TNP-470, marimastat and the tubulin-binding agent Ang-510. Biochem Biophys Res Commun. 2010 Jan 8;391(2):1161-5. [Content Brief]

[4]. Skipper JB, et al. In vivo efficacy of marimastat and chemoradiation in head and neck cancer xenografts. ORL J Otorhinolaryngol Relat Spec. 2009;71(1):1-5. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	3.0174 mL	15.0871 mL	30.1741 mL	75.4353 mL
	5 mM	0.6035 mL	3.0174 mL	6.0348 mL	15.0871 mL
	10 mM	0.3017 mL	1.5087 mL	3.0174 mL	7.5435 mL
	15 mM	0.2012 mL	1.0058 mL	2.0116 mL	5.0290 mL
	20 mM	0.1509 mL	0.7544 mL	1.5087 mL	3.7718 mL
	25 mM	0.1207 mL	0.6035 mL	1.2070 mL	3.0174 mL
	30 mM	0.1006 mL	0.5029 mL	1.0058 mL	2.5145 mL
	40 mM	0.0754 mL	0.3772 mL	0.7544 mL	1.8859 mL
	50 mM	0.0603 mL	0.3017 mL	0.6035 mL	1.5087 mL
	60 mM	0.0503 mL	0.2515 mL	0.5029 mL	1.2573 mL
	80 mM	0.0377 mL	0.1886 mL	0.3772 mL	0.9429 mL
	100 mM	0.0302 mL	0.1509 mL	0.3017 mL	0.7544 mL

Bioz

Keywords

Marimastat

22 Cited Publications

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Marimastat

Publications Citing Use of MedChemExpress (MCE) Marimastat

Alle MMP Isoform-spezifische Produkte anzeigen