Marimastat (BB-2516)

For research use only.

Catalog No.S7156 Synonyms: TA2516

7 publications

Marimastat (BB-2516) Chemical Structure

CAS No. 154039-60-8

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.

Selleck's Marimastat (BB-2516) has been cited by 7 publications

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  • (E, F) Uev1A mediates negative feedback of NF-κB signaling pathway is dependent on TACE activity. Forty-eight hours after transfection, the cells were pre-treated with BB-2516 (20 μM) for 1 h, followed by TNFα (40 ng/ml) treatment for 2 h. Cell was fixed and stained with antibodies against HA and p65. The same cells were also stained with DAPI to reveal nuclei. White arrows indicate UEV1A-overexpressed cells. (F) Quantitative analysis of the experiments shown in (E). Percentage of cells displaying nuclear p65 is shown for UEV1A- overexpressed or vector-transfected cells. Each sample contains about 1000 cells. The significance of differences was assessed by two-tailed Student's test (***P < 0.001).

    Cell Signal, 2018, 42:155-164. Marimastat (BB-2516) purchased from Selleck.

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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.
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)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT1080 NH;pOIhHfW6ldHnvckBie3OjeR?= NF25R|BKdiC4aYTyc{BqdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhdWG2cnn4JI1mfGGubH;wdo91\WG|ZTCyJIl{d2yjdHXkJIZzd21iaIXtZY4hUFRzMEiwJIZq[nKxc3HyZ49u[SClZXzsd{BqdmS3Y3XkJJdqfGhiVF7GMEBKSzVyPUCuNFAxQDYQvF2u NG\2boE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi97OEezO|EzLz57OEezO|EzRC:jPh?=
THP-1 NFfkZ3FHfW6ldHnvckBie3OjeR?= MXTT[Yxm[3SrdnWgbY5pcWKrdHnvckBw\iC2aHWgZ4VtdHWuYYKgWG5HKGGucHjhJJJmdGWjc3Wg[pJwdSCOUGOtd5RqdXWuYYTl[EBVUFBvMTDj[YxteyxiSVO1NF0zNjIQvF2u MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTd3NEW5N{c,OTF5NUS1PVM9N2F-
Sf9 NI\NO21HfW6ldHnvckBie3OjeR?= NXjnSXhTPiCqcoO= NVWyb3VZUW6qaXLpeIlwdiCxZjDmeYxtKGynbnf0bEBz\WOxbXLpcoFvfCCDRFHNWHM1KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIHnud4VkfCCVZkmgZ4VtdHNiYX\0[ZIhPiCqcoOgZpkh[WytYXzpcoUheGixc4DoZZRie2VvYnHz[YQh[XO|YYmsJGlEPTB;MUFOwG0v NW\welBxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVM4OzVpPkK2OlU{PzN3PD;hQi=>
Sf9 NIPQUINHfW6ldHnvckBie3OjeR?= NEn5b2c3KGi{cx?= MXTJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIILlZ49u[mmwYX70JGFFSU2WU{WgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hcW6|ZXP0JHNnQSClZXzsd{Bi\nSncjC2JIhzeyCkeTDhcItidGmwZTDwbI9{eGijdHHz[U1j[XOnZDDhd5NigSxiSVO1NF0yOM7:TT6= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3M{ezOUc,OjZ4NUO3N|U9N2F-
A549 MV7GeY5kfGmxbjDhd5NigQ>? MmXWNVAhfU1? MmS2NUBpeg>? NYDVcVQyUW6qaXLpeIlwdiCxZjDBSGFOOTBiaX6gbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHLleIFk\WyudXzpckB{cGWmZHnu[{BifCBzMDD1UUBi\nSncjCxJIhzKGK7IFXMTXNC MmHMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzOUKwNlMoRjJ4MUmyNFI{RC:jPh?=
A549 NIP5VIlHfW6ldHnvckBie3OjeR?= MoHHNVAhfU1? M3K2XVEhcHJ? M33oRWlvcGmkaYTpc44hd2ZiQVTBUVE4KGmwIHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hWE2DLYP0bY12dGG2ZXSgd49tfWKuZTDUS2ZidHCqYTDs[ZZmdCCrbjDj[YxtKHO3cHXycoF1[W62IHH0JFExKHWPIIDy[Ylv[3WkYYTl[EBnd3JiMTDodkBnd2yub4fl[EBjgSCSTVGgd5RqdXWuYYTpc44hdWWjc4Xy[YQh[W[2ZYKgNUBpeiCkeTDFUGlUSQ>? NVPOXXFmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xPVIxOjNpPkK2NVkzODJ|PD;hQi=>

... Click to View More Cell Line Experimental Data

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]


Kinase Assay:[2]
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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 Research:[5]
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  • Animal Models: Orthotopic oral squamous cell carcinoma implantation model
  • Dosages: 150 mg/kg/day
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 54 mg/mL (162.94 mM)
Water Insoluble
Ethanol '7 mg/mL warmed
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.

* 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.

Chemical Information

Molecular Weight 331.41


CAS No. 154039-60-8
Storage powder
in solvent
Synonyms TA2516
Smiles CC(C)CC(C(C(=O)NO)O)C(=O)NC(C(=O)NC)C(C)(C)C

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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MMP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID