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MMP-13 Inhibitor (Synonyms: Collagenase-3 Inhibitor,Matrix Metalloproteinase-13 Inhibitor,4,6-Pyrimidinedicarboxamide)

Catalog No.GC17245

MMP-13 Inhibitor (compound 4) is a potent, highly selective, non-zinc-chelating MMP-13 inhibitor with an IC50 of 8 nM.

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MMP-13 Inhibitor Chemical Structure

Cas No.: 544678-85-5

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1mg
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5mg
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10mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: 8 nM

MMP-13 Inhibitor is a MMP-13 inhibitor.

Matrix metalloproteinases (MMPs), a family of zinc endopeptidases, can degrade proteins of the extracellular matrix, such as collagens, elastins, matrix glycoproteins, and proteoclycans. Zymogen activation and endogenous tissue inhibitors of matrix metalloproteinases control MMP activity during normal morphogenesis and tissue homeostasis. Abnormal expression or activity of MMPs has been reported to be related with pathological processes including metastasis, angiogenesis, cardiovascular disease, and rheumathoid arthritis and osteoarthritis.

In vitro: MMP-13 Inhibitor was previously synthesized as a pyrimidine dicarboxamide that could inhibit the matrix metalloproteinase-13 (MMP-13) with the IC50 of 8 nM. Moreover, MMP-13 Inhibitor was found to be able to bind to MMP pockets that are unique to MMP-13 rather than the catalytic zinc, and therefore was specific for MMP-13 over other MMPs. In addition, during endochondral ossification, MMP-13 Inhibitor could also block osterix-dependent calcification of matrices in limb bud cells [1, 2, 3].

In vivo: So far, there is no animal in vivo study reported.

Clinical trial: So far, no clinical study has been conducted.

References:
1.  Carrascal, N.A. and Rizzo, R.C. Calculation of binding free energies for non-zinc chelating pyrimidine dicarboxamide inhibitors with MMP-13. Bioorg.Med.Chem.Lett. 19(1), (2009).
2.  Engel, C.K.,Pirard, B.,Schimanski, S., et al. Structural basis for the highly selective inhibition of MMP-13. Chem.Biol. 12(2), 181-189 (2005).
3.  Nishimura, R.,Wakabayashi, M.,Hata, K., et al. Osterix regulates calcification and degradation of chondrogenic matrices through matrix metalloproteinase 13 (MMP13) expression in association with transcription factor Runx2 during endochondral ossification. J.Biol.Chem. 287(40), 33179-33190 (2012).

Chemical Properties

Cas No. 544678-85-5 SDF
Synonyms Collagenase-3 Inhibitor,Matrix Metalloproteinase-13 Inhibitor,4,6-Pyrimidinedicarboxamide
Chemical Name N4,N6-bis[(4-fluoro-3-methylphenyl)methyl]-4,6-pyrimidinedicarboxamide
Canonical SMILES FC1=C(C)C=C(CNC(C2=CC(C(NCC3=CC=C(F)C(C)=C3)=O)=NC=N2)=O)C=C1
Formula C22H20F2N4O2 M.Wt 410.4
Solubility ≤0.5mg/ml in ethanol;2mg/ml in DMSO;2mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.4366 mL 12.1832 mL 24.3665 mL
5 mM 0.4873 mL 2.4366 mL 4.8733 mL
10 mM 0.2437 mL 1.2183 mL 2.4366 mL
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