| Catalog No. | HV374026 |
|---|
| Species reactivity | Human |
|---|
| Applications | ELISA, Bioactivity: FACS, Functional assay, Research in vivo |
|---|
| Host species | Human |
|---|
| Isotype | IgG |
|---|
| Clone ID | GSK2394002 |
|---|
| Biological activity |
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]. GSK2394002 (systemic) inhibits surgically induced murine osteoarthritis progression but causes severe, long-lasting cardiovascular side effects in cynomolgus monkeys [3]. |
| Expression system |
Mammalian cells |
| Clonality |
Monoclonal |
| Target |
ADAMTS11, ADAM-TS 11, A disintegrin and metalloproteinase with thrombospondin motifs 11, ADAMTS-11, ADMP2, ADAM-TS 5, ADAMTS-5, ADMP-2, ADAMTS5, Aggrecanase-2, ADAM-TS5, A disintegrin and metalloproteinase with thrombospondin motifs 5 |
| Endotoxin level |
Please contact the lab for this information. |
| Purity |
>95% purity as determined by SDS-PAGE. |
| Purification |
Protein A/G purified from cell culture supernatant. |
| Accession |
Q9UNA0 |
| Form |
Liquid |
| Storage buffer |
0.01M PBS pH 7.4 Please refer to the specific buffer information in the hardcopy of datasheet or the lot-specific COA.
|
| Stability and Storage |
Use a manual defrost freezer and avoid repeated freeze thaw cycles. Store at 2 to 8°C for frequent use. Store at -20 to -80°C for twelve months from the date of receipt. |
| Alternate Names | GSK2394002 |
|---|
| Background | A disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS5) is a ~101 kDa protein. Metalloproteinase that plays an important role in connective tissue organization, development, inflammation and cell migration. Extracellular matrix (ECM) degrading enzyme that show proteolytic activity toward the hyalectan group of chondroitin sulfate proteoglycans (CSPGs) including ACAN, VCAN, BCAN and NCAN. Cleavage within the hyalectans occurs at Glu-Xaa recognition motifs. Plays a role in embryonic development, including limb and cardiac morphogenesis, and skeletal muscle development through its VCAN remodeling properties. Cleaves VCAN in the pericellular matrix surrounding myoblasts, facilitating myoblast contact and fusion which is required for skeletal muscle development and regeneration. 1. Nakada, M. et al. (2005) Acta neuropathologica 110, 239-46. PMID: 161335472. Longpré, JM. et al. (2009) The international journal of biochemistry & cell biology 41, 1116-26. PMID: 18992360 |
|---|
| References |
1. Apte SS, et al. Anti-ADAMTS5 monoclonal antibodies: implications for aggrecanase inhibition in osteoarthritis. Biochem J. 2016;473(1):e1-e4. [HV374026]
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. [HV374026]
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. [HV374026]
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. View More [HV374026] |
| Note |
For research use only. Not suitable for clinical or therapeutic use. |
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