Marimastat (BB-2516)

Catalog No.S7156 Batch:S715602

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Technical Data

Formula

C15H29N3O5
Molecular Weight 331.41 CAS No. 154039-60-8
Solubility (25°C)* In vitro DMSO 54 mg/mL (162.94 mM)
Ethanol 7 mg/mL (21.12 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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)		 View More
3 nM 5 nM 6 nM 9 nM 16 nM
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]
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]

Protocol (from reference)

Kinase Assay:

[2]
  • 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.

Animal Study:

[5]
  • Animal Models

    Orthotopic oral squamous cell carcinoma implantation model

  • Dosages

    150 mg/kg/day

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Cell Signal, 2018, 42:155-164]

Selleck's Marimastat (BB-2516) has been cited by 18 publications

CD26-negative and CD26-positive tissue-resident fibroblasts contribute to functionally distinct CAF subpopulations in breast cancer [ Nat Commun, 2023, 14(1):183] PubMed: 36635273
Chronic kidney disease causes blood-brain barrier breakdown via urea-activated matrix metalloproteinase-2 and insolubility of tau protein [ Aging (Albany NY), 2023, 15(20):10972-10995] PubMed: 37889501
Cell-matrix interface regulates dormancy in human colon cancer stem cells [ Nature, 2022, 10.1038/s41586-022-05043-y] PubMed: 35798028
Hotspot ESR1 mutations are multimodal and contextual modulators of breast cancer metastasis [ Cancer Res, 2022, canres.CAN-21-2576-E.2021] PubMed: 35078818
Transforming growth factor β1 signaling links extracellular matrix remodeling to intracellular lipogenesis upon physiological feeding events [ J Biol Chem, 2022, 298(4):101748] PubMed: 35189145
Evaluation of the matrix metalloproteinase 9 (MMP9) inhibitor Andecaliximab as an Anti-invasive therapeutic in Head and neck squamous cell carcinoma [ Oral Oncol, 2022, 132:106008] PubMed: 35803110
Marimastat alleviates oxidative stress induced cellular senescence by activating autophagy [ Biochem Biophys Res Commun, 2022, 620:121-128] PubMed: 35780580
Lymphocyte access to lymphoma is impaired by high endothelial venule regression [ Cell Rep, 2021, 37(4):109878] PubMed: 34706240
EPB41L5 controls podocyte extracellular matrix assembly by adhesome-dependent force transmission [ Cell Rep, 2021, 34(12):108883] PubMed: 33761352
Transcriptional networks identify synaptotagmin-like 3 as a regulator of cortical neuronal migration during early neurodevelopment [ Cell Rep, 2021, 34(9):108802] PubMed: 33657377

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.