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Cat. No.: HY-P992358

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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.

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

GSK2394002 Chemical Structure

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Species Reactivity
- In Vitro
- In Vivo
- Gene ID
- Accession
- Target
- Conjugated
- Reconsititution
- Format
- Application
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Species Reactivity

Human

In Vitro

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.

In Vivo

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.

Gene ID

11096 [NCBI]

Accession

Q9UNA0

Target

ADAMTS5

Conjugated

Unconjugated

Reconsititution

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

Format

Product Image

Application

ELISA, FACS, Functional assay

Chemical Information

Formulation

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

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

Pureté et documentation

Inhibitory Antibodies User Guide (603 KB)

Références

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

[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. [Content Brief]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Minimum order quantity

100 mg

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Activité biologique
- Description
- Species Reactivity
- In Vitro
- In Vivo
- Gene ID
- Accession
- Target
- Conjugated
- Reconsititution
- Format
- Application
Chemical Information
Pureté et documentation
Références

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MCE Japan Authorized Agent:

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GSK2394002

DPBS Buffer (1×)

Cytotoxicity LDH Assay Kit

PBS Buffer (1×)

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

GSK2394002 Related Classifications

HY-P992358 Related Classifications