Marimastat (BB-2516)

Catalog No.S7156 Synonyms: TA2516

For research use only.

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

CAS No. 154039-60-8

Selleck's Marimastat (BB-2516) has been cited by 12 Publications

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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)
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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 Ml3KSpVv[3Srb36gZZN{[Xl? M37tdGlvKH[rdILvJIlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBu[XS{aYigcYV1[Wyub4Dyc5Rm[XOnIEKgbZNwdGG2ZXSg[pJwdSCqdX3hckBJXDFyOECg[oljem:|YYLjc41iKGOnbHzzJIlv\HWlZXSge4l1cCCWTl[sJGlEPTB;MD6wNFA5Pc7:TT6= NYe1dJhXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUi3N|cyOid-OUi3N|cyOjxxYU6=
THP-1 MojRSpVv[3Srb36gZZN{[Xl? MXvT[Yxm[3SrdnWgbY5pcWKrdHnvckBw\iC2aHWgZ4VtdHWuYYKgWG5HKGGucHjhJJJmdGWjc3Wg[pJwdSCOUGOtd5RqdXWuYYTl[EBVUFBvMTDj[YxteyxiSVO1NF0zNjIQvF2u NXfHenJURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUG3OVQ2QTNpPkGxO|U1PTl|PD;hQi=>
Sf9 NVPPfXNWTnWwY4Tpc44h[XO|YYm= MnTtOkBpenN? NGnHeWJKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJJJm[2:vYnnuZY51KEGGQV3UV|QhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iaX7z[YN1KFOoOTDj[YxteyCjZoTldkA3KGi{czDifUBidGujbHnu[UBxcG:|cHjheIF{\S2kYYPl[EBie3OjeTygTWM2OD1zMN88UU4> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3M{ezOUc,OjZ4NUO3N|U9N2F-
Sf9 MV3GeY5kfGmxbjDhd5NigQ>? MlTKOkBpenN? M1\0WWlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigdoVkd22kaX7hcpQhSUSDTWTTOUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCrboPlZ5QhW2Z7IHPlcIx{KGGodHXyJFYhcHK|IHL5JIFtc2GuaX7lJJBpd3OyaHH0ZZNmNWKjc3XkJIF{e2G7LDDJR|UxRTFyzszNMi=> NUfT[3BbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVM4OzVpPkK2OlU{PzN3PD;hQi=>
A549 MYTGeY5kfGmxbjDhd5NigQ>? M1nzb|ExKHWP NYHa[GdEOSCqch?= NU\1RW5xUW6qaXLpeIlwdiCxZjDBSGFOOTBiaX6gbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHLleIFk\WyudXzpckB{cGWmZHnu[{BifCBzMDD1UUBi\nSncjCxJIhzKGK7IFXMTXNC NWDId3h2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xPVIxOjNpPkK2NVkzODJ|PD;hQi=>
A549 M1voS2Z2dmO2aX;uJIF{e2G7 MofXNVAhfU1? NEXEdGwyKGi{ NHW2No9KdmirYnn0bY9vKG:oIFHERW0yPyCrbjDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKFCPQT3zeIlufWyjdHXkJJNwdHWkbHWgWGdH[WyyaHGgcIV3\WxiaX6gZ4VtdCC|dYDldo5ifGGwdDDheEAyOCC3TTDwdoVqdmO3YnH0[YQh\m:{IEGgbJIh\m:ubH;3[YQh[nliUF3BJJN1cW23bHH0bY9vKG2nYYP1doVlKGGodHXyJFEhcHJiYomgSWxKW0F? NIj1[o89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkG5NlAzOyd-Mk[xPVIxOjN:L3G+
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 Research:[5]
  • Animal Models: Orthotopic oral squamous cell carcinoma implantation model
  • Dosages: 150 mg/kg/day
  • Administration: p.o.

Solubility (25°C)

In vitro

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.


Chemical Information

Molecular Weight 331.41


CAS No. 154039-60-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)CC(C(C(=O)NO)O)C(=O)NC(C(=O)NC)C(C)(C)C

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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