Bioactivity | 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]. | ||||||||||||
Invitro | ADAMTS-5 (aggrecanase-2) is an extracellular matrix-degrading protease implicated in cartilage destruction in arthritis[2]. | ||||||||||||
Name | ADAMTS-5 Inhibitor | ||||||||||||
CAS | 929634-33-3 | ||||||||||||
Formula | C16H11ClF3N3OS3 | ||||||||||||
Molar Mass | 449.92 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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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. |