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 9 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.
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

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 NWCxcoJxTnWwY4Tpc44h[XO|YYm= NVG3R4xVUW5idnn0do8hcW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KG2jdILpfEBu\XSjbHzvdJJwfGWjc3WgNkBqe2:uYYTl[EBnem:vIHj1cYFvKEiWMUC4NEBncWK{b4PhdoNwdWFiY3XscJMhcW6mdXPl[EB4cXSqIGTOSkwhUUN3ME2wMlAxODh3zszNMi=> NX7BcIJxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUi3N|cyOid-OUi3N|cyOjxxYU6=
THP-1 Ml\MSpVv[3Srb36gZZN{[Xl? MUTT[Yxm[3SrdnWgbY5pcWKrdHnvckBw\iC2aHWgZ4VtdHWuYYKgWG5HKGGucHjhJJJmdGWjc3Wg[pJwdSCOUGOtd5RqdXWuYYTl[EBVUFBvMTDj[YxteyxiSVO1NF0zNjIQvF2u NX25VWJ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUG3OVQ2QTNpPkGxO|U1PTl|PD;hQi=>
Sf9 M4[zPGZ2dmO2aX;uJIF{e2G7 NVv1cIpbPiCqcoO= MlvuTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBCTEGPVGO0JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKGmwc3XjeEBU\jliY3XscJMh[W[2ZYKgOkBpenNiYomgZYxs[WyrbnWgdIhwe3CqYYThd4Uu[mG|ZXSgZZN{[XluIFnDOVA:OTEQvF2u M4TSWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWzO|M2Lz5{Nk[1N|c{PTxxYU6=
Sf9 Mon1SpVv[3Srb36gZZN{[Xl? M1PEVlYhcHK| MnzHTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBCTEGPVGO1JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKGmwc3XjeEBU\jliY3XscJMh[W[2ZYKgOkBpenNiYomgZYxs[WyrbnWgdIhwe3CqYYThd4Uu[mG|ZXSgZZN{[XluIFnDOVA:OTEQvF2u NILZ[I49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1N|c{PSd-Mk[2OVM4OzV:L3G+
A549 M2j3c2Z2dmO2aX;uJIF{e2G7 MkTVNVAhfU1? M4nUblEhcHJ? M2C3eWlvcGmkaYTpc44hd2ZiQVTBUVExKGmwIHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCkZYThZ4VtdHWuaX6gd4hm\GSrbnegZZQhOTBidV2gZYZ1\XJiMTDodkBjgSCHTFnTRS=> NEm2Tnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkG5NlAzOyd-Mk[xPVIxOjN:L3G+
A549 NFn2PINHfW6ldHnvckBie3OjeR?= NIS3OVMyOCC3TR?= M362fVEhcHJ? NWLpN|ZPUW6qaXLpeIlwdiCxZjDBSGFOOTdiaX6gbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCSTVGtd5RqdXWuYYTl[EB{d2y3YnzlJHRITmGucHjhJIxmfmWuIHnuJINmdGxic4Xw[ZJv[XSjboSgZZQhOTBidV2gdJJmcW6ldXLheIVlKG[xcjCxJIhzKG[xbHzve4VlKGK7IGDNRUB{fGmvdXzheIlwdiCvZXHzeZJm\CCjZoTldkAyKGi{IHL5JGVNUVOD MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjF7MkCyN{c,OjZzOUKwNlM9N2F-
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.
  • (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):
50% DMSO+PBS
For best results, use promptly after mixing.

30mg/mL

* 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
Formula

C15H29N3O5

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

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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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