Home Proteases MMP inhibitor Marimastat (BB-2516) For research use only.

Marimastat (BB-2516)

Synonyms: TA2516

Marimastat (BB-2516, TA2516) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7 with IC50 of 3 nM, 5 nM, 6 nM, 9 nM and 13 nM, respectively. Phase 3.

Marimastat (BB-2516) Chemical Structure

Marimastat (BB-2516) Chemical Structure

CAS No. 154039-60-8

Purity & Quality Control

Marimastat (BB-2516) Related Products

Signaling Pathway

MMP Signaling Pathways

MMP Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT1080 Function assay In vitro inhibitory activity against matrix metalloprotease 2 isolated from human HT1080 fibrosarcoma cells induced with TNF, IC50=0.00085μM. 9873712
THP-1 Function assay Selective inhibition of the cellular TNF alpha release from LPS-stimulated THP-1 cells, IC50=2.1μM. 11754593
Sf9 Function assay 6 hrs Inhibition of full length recombinant ADAMTS4 (unknown origin) expressed in insect Sf9 cells after 6 hrs by alkaline phosphatase-based assay, IC50=10μM. 26653735
Sf9 Function assay 6 hrs Inhibition of full length recombinant ADAMTS5 (unknown origin) expressed in insect Sf9 cells after 6 hrs by alkaline phosphatase-based assay, IC50=10μM. 26653735
A549 Function assay 10 uM 1 hr Inhibition of ADAM10 in human A549 cells assessed as inhibition of betacellulin shedding at 10 uM after 1 hr by ELISA 26192023
A549 Function assay 10 uM 1 hr Inhibition of ADAM17 in human A549 cells assessed as decrease in PMA-stimulated soluble TGFalpha level in cell supernatant at 10 uM preincubated for 1 hr followed by PMA stimulation measured after 1 hr by ELISA 26192023
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Biological Activity

Description Marimastat (BB-2516, TA2516) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7 with IC50 of 3 nM, 5 nM, 6 nM, 9 nM and 13 nM, respectively. Phase 3.
Targets
MMP-9 [1]
(cell-free assay)		 MMP-1 [1]
(cell-free assay)		 MMP-2 [1]
(cell-free assay)		 MMP-14 [1]
(cell-free assay)		 MMP-7 [1]
(cell-free assay)		 Click to View More Targets
3 nM 5 nM 6 nM 9 nM 16 nM
In vitro
In vitro

Marimastat (100 nM) significantly inhibits the expression of MMP14 in U251, U87, GBM39, and GBM43 tumor cells. Marimastat specifically inhibits the growth of glioma cells and has no effect on normal human astrocytes (NHA).[3]

Marimastat early down-regulates the expression of Notch target genes, such as Hes1 and Hes5.[4]
Kinase Assay Inhibitor kinetics
Recombinant human MMP2 is activated with 1 mM of 4-aminophenylmercuric acetate for 1 hour at 37°C. Rates of cleavage of 1 μM of the quenched fluorescent MMP substrate (7-methoxycoumarin-4-yl)acetyl-Pro-Leu-Gly-Leu-[3-(2,4-dinitrophenyl)-L-2,3-diaminoproprionyl]-Ala-Arg-NH2 are measured in 96-well fluorimetry plates at 37°C 100 mM Tris-HCl (pH 7.5), 100 mM NaCl, 10 mM CaCl2, 0.05% Brij 35 using a 320 nm excitation filter and a 405 nm emission filter in the presence of increasing inhibitor concentrations. Curve-fitting and IC50 calculations are done using GraphPad Prism 5.0 Software.
In Vivo
In vivo

In an orthotopic oral squamous cell carcinoma implantation model, marimastat (150 mg/kg/day, p.o.) administered by an osmotic pump significantly suppresses the cervical lymph node metastasis and activation of MMP-2, and has a significantly better survival than control group.[5]

Marimastat reduces MMP hyperactivity of polycystic human and rat cholangiocytes and blocks the cystic expansion of PCK cholangiocytes. Chronic treatment of 8-week-old PCK rats with marimastat inhibits hepatic cystogenesis and fibrosis.[6]
Animal Research Animal Models Orthotopic oral squamous cell carcinoma implantation model
Dosages 150 mg/kg/day
Administration p.o.

Chemical Information & Solubility

Molecular Weight 331.41 Formula

C15H29N3O5
CAS No. 154039-60-8 SDF Download Marimastat (BB-2516) SDF
Smiles CC(C)CC(C(C(=O)NO)O)C(=O)NC(C(=O)NC)C(C)(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 54 mg/mL ( (162.94 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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