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MMP-13 Inhibitor
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MMP-13 Inhibitor图片
CAS NO:544678-85-5
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
MMP-13 Inhibitor (compound 4) 是一种有效的、高选择性的、非锌螯合的 MMP-13 抑制剂，IC50 为 8 nM。
Cas No.544678-85-5
别名N4,N6-双(4-氟-3-甲基苄基)嘧啶-4,6-二甲酰胺,Collagenase-3 Inhibitor,Matrix Metalloproteinase-13 Inhibitor,4,6-Pyrimidinedicarboxamide
化学名N4,N6-bis[(4-fluoro-3-methylphenyl)methyl]-4,6-pyrimidinedicarboxamide
Canonical SMILESFC1=C(C)C=C(CNC(C2=CC(C(NCC3=CC=C(F)C(C)=C3)=O)=NC=N2)=O)C=C1
分子式C22H20F2N4O2
分子量410.4
溶解度≤0.5mg/ml in ethanol;2mg/ml in DMSO;2mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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).