MMP-13 Inhibitor
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 410.4 |
Cas No. | 544678-85-5 |
Formula | C22H20F2N4O2 |
Synonyms | Collagenase-3 Inhibitor,Matrix Metalloproteinase-13 Inhibitor,4,6-Pyrimidinedicarboxamide |
Solubility | ≤0.5mg/ml in ethanol;2mg/ml in DMSO;2mg/ml in dimethyl formamide |
Chemical Name | N4,N6-bis[(4-fluoro-3-methylphenyl)methyl]-4,6-pyrimidinedicarboxamide |
SDF | Download SDF |
Canonical SMILES | FC1=C(C)C=C(CNC(C2=CC(C(NCC3=CC=C(F)C(C)=C3)=O)=NC=N2)=O)C=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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