For research use only. Not for therapeutic Use.
ADAMTS-5 Inhibitor is a potent ADAMTS-5 (aggrecanase-2) inhibitor, with an IC50 of 1.1 µM. ADAMTS-5 Inhibitor shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1)[1].
ADAMTS-5 (aggrecanase-2) is an extracellular matrix-degrading protease implicated in cartilage destruction in arthritis[2].
Catalog Number | R026137 |
CAS Number | 929634-33-3 |
Synonyms | (5Z)-5-[[5-[(4-chlorophenyl)methylsulfanyl]-1-methyl-3-(trifluoromethyl)pyrazol-4-yl]methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one |
Molecular Formula | C16H11ClF3N3OS3 |
Purity | ≥95% |
InChI | InChI=1S/C16H11ClF3N3OS3/c1-23-14(26-7-8-2-4-9(17)5-3-8)10(12(22-23)16(18,19)20)6-11-13(24)21-15(25)27-11/h2-6H,7H2,1H3,(H,21,24,25)/b11-6- |
InChIKey | CVYPRDPBCXSVBN-WDZFZDKYSA-N |
SMILES | CN1C(=C(C(=N1)C(F)(F)F)C=C2C(=O)NC(=S)S2)SCC3=CC=C(C=C3)Cl |
Reference | [1]. Gilbert AM, et al. 5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1189-92. [2]. Wylie JD, et al. Adamts5 (aggrecanase-2) is widely expressed in the mouse musculoskeletal system and is induced in specific regions of knee joint explants by inflammatory cytokines. J Orthop Res. 2012 Feb;30(2):226-33. |