GSK2394002 

GSK2394002 is an antibody inhibitor targeting ADAMTS-4 and ADAMTS-5, with cartilage-penetrating ability following systemic administration. GSK2394002 inhibits the release of aggrecan-derived neoepitopes and reduces cartilage degradation, exhibiting the potential to relieve pain, alleviate hyperalgesia and inhibit the progression of joint damage. GSK2394002 also induces potentially irreversible cardiovascular effects such as increased mean arterial pressure and myocardial ischemia in cynomolgus monkeys^[1][2][3][4].

Human

GSK2394002 effectively suppresses ADAMTS5-mediated aggrecan cleavage, as measured by reduced ARGS epitope release, from human knee cartilage explants^[1].
GSK2394002 binds an epitope spanning the catalytic and disintegrin-like modules of ADAMTS5 and inhibits its activity via an allosteric lock effect on the enzyme's active site^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GSK2394002 (systemic) inhibits surgically induced murine osteoarthritis progression but causes severe, long-lasting cardiovascular side effects in cynomolgus monkeys^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

11096  [NCBI]

Q9UNA0

ADAMTS5

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

Please refer to the lot-specific COA for specific buffer information.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Apte SS, et al. Anti-ADAMTS5 monoclonal antibodies: implications for aggrecanase inhibition in osteoarthritis. Biochem J. 2016;473(1):e1-e4.

  [2]. Larkin J, Lohr T, Elefante L, et al. The highs and lows of translational drug development: antibody-mediated inhibition of ADAMTS-5 for osteoarthritis disease modification[J]. Osteoarthritis and Cartilage, 2014, 22: S483-S484.

  [3]. Bondeson J, Wainwright S, Hughes C E, et al. Can allosteric inhibitors of adamts4 and adamts5 prevent osteoarthritis disease progression[J]. History, 2015, 10(23): 5-14.

  [4]. Jiang P, et al. A brief review of current treatment options for osteoarthritis including disease-modifying osteoarthritis drugs (DMOADs) and novel therapeutics. Ann Med Surg (Lond). 2024;86(7):4042-4048. Published 2024 Jun 4.