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BOC Sciences |
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Alabiotech Inc. |
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Nextpeptide Inc |
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| | MMP-8 INHIBITOR I Basic information |
| Product Name: | MMP-8 INHIBITOR I | | Synonyms: | (3R)-(+)-[2-(4-METHOXYBENZENESULFONYL)-1,2,3,4-TETRAHYDROISOQUINOLINE-3-HYDROXAMATE];MMP-8 INHIBITOR I;MMP 8-I;3-Isoquinolinecarboxamide, 1,2,3,4-tetrahydro-N-hydroxy-2-[(4-methoxyphenyl)sulfonyl]-, (3R)-;MMP-8 Inhibitor I (Matrix Metalloproteinase-8 Inhibitor I) | | CAS: | 236403-25-1 | | MF: | C17H18N2O5S | | MW: | 362.4 | | EINECS: | | | Product Categories: | | | Mol File: | Mol File |  |
| | MMP-8 INHIBITOR I Chemical Properties |
| storage temp. | -20°C | | solubility | Chloroform (Slightly), Methanol (Slightly) | | form | Solid | | color | Off-White to Light Yellow | | InChI | InChI=1S/C17H18N2O5S/c1-24-14-6-8-15(9-7-14)25(22,23)19-11-13-5-3-2-4-12(13)10-16(19)17(20)18-21/h2-9,16,21H,10-11H2,1H3,(H,18,20)/t16-/m1/s1 | | InChIKey | PPELJLBDXLMTEW-MRXNPFEDSA-N | | SMILES | C1C2=C(C=CC=C2)C[C@H](C(NO)=O)N1S(C1=CC=C(OC)C=C1)(=O)=O |
| | MMP-8 INHIBITOR I Usage And Synthesis |
| Description | MMP-8 Inhibitor I is a selective inhibitor of the neutrophil collagenase matrix metalloproteinase-8 (MMP-8) with an IC50 value of 4 nM. This inhibitor does not target the activities of other MMPs in vitro. MMP-8 cleaves interstitial collagens and has exhibited activity in atherosclerotic plaques, angiogenesis, and stem cell mobilization. Additionally, MMP-8 expression is observed in normal mammary epithelial cells, whereas a loss of expression is observed in human ductal carcinoma in situ and the deletion of MMP-8 accelerates tumor onset in a mouse model of aggressive breast cancer. | | Uses | MMP 8-I is a matrix metalloproteinase 8 inhibitor. Matrix metalloproteinases are involved with tight junction protein degradation in endothelial cells. | | in vivo | MMP-8 inhibitor-1 (compound 21) (100 mg/kg, orally) has not significant oral bioavailability, with maximal plasma levels (Cmax) of only 2.3 mg/mL[1]. | | IC 50 | MMP-8 | | References | [1] HANS MATTER. Tetrahydroisoquinoline-3-carboxylate based matrix-metalloproteinase inhibitors: design, synthesis and structure–activity relationship[J]. Bioorganic & Medicinal Chemistry, 2002, 10 11: Pages 3529-3544. DOI: 10.1016/s0968-0896(02)00215-8
[2] MCNULTY A, WEINBERG B J, GUILAK F. Inhibition of Matrix Metalloproteinases Enhances In Vitro Repair of the Meniscus[C]//38 1. 2009: 0. DOI: 10.1007/s11999-008-0596-6
[3] GERALD W PRAGER. Vascular endothelial growth factor (VEGF) induces rapid prourokinase (pro-uPA) activation on the surface of endothelial cells.[J]. Blood, 2004, 103 3: 955-962. DOI: 10.1182/blood-2003-07-2214
[4] QISHAN CHEN. Matrix metalloproteinases: inflammatory regulators of cell behaviors in vascular formation and remodeling.[J]. Mediators of Inflammation, 2013: 928315. DOI: 10.1155/2013/928315
[5] JULIE DECOCK. Pleiotropic functions of the tumor- and metastasis-suppressing matrix metalloproteinase-8 in mammary cancer in MMTV-PyMT transgenic mice.[J]. Breast Cancer Research: BCR, 2015: 38. DOI: 10.1186/s13058-015-0545-8
[6] MUGE SARPER. Loss of MMP-8 in ductal carcinoma in situ (DCIS)-associated myoepithelial cells contributes to tumour promotion through altered adhesive and proteolytic function.[J]. Breast Cancer Research: BCR, 2017: 33. DOI: 10.1186/s13058-017-0822-9 |
| | MMP-8 INHIBITOR I Preparation Products And Raw materials |
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