ADAMTS

Adamalysin-like metalloproteinase with thrombospondin motifs

ADAMTS is a class of zinc-dependent secreted metalloproteases that primarily participate in extracellular matrix (ECM) degradation and remodeling, blood coagulation regulation, and cardiovascular homeostasis. This family consists of 19 ADAMTS proteases and 7 ADAMTS-like proteins, each with distinct biological functions. Among them, ADAMTS1, 4, and 5 are responsible for proteoglycan degradation, ADAMTS2, 3, and 14 facilitate procollagen processing, ADAMTS13 regulates coagulation by cleaving von Willebrand factor (vWF), and ADAMTS7 and 12 influence vascular smooth muscle cell migration, contributing to atherosclerosis. Additionally, ADAMTS1 and ADAMTS8 function as tumor suppressors, inhibiting angiogenesis and thereby restricting tumor growth. Dysregulation of ADAMTS functions is associated with various diseases. For example, mutations in ADAMTS2 lead to Ehlers-Danlos syndrome (a connective tissue disorder with skin hyperelasticity) due to impaired collagen maturation; excessive ADAMTS5 activity disrupts proteoglycan homeostasis and exacerbates osteoarthritis; ADAMTS13 deficiency causes thrombotic thrombocytopenic purpura (TTP), resulting in abnormal blood clot formation. Additionally, ADAMTS7 promotes vascular remodeling, accelerating atherosclerosis progression. Therefore, selective inhibitors or activators targeting ADAMTS have emerged as potential therapeutic strategies for joint diseases, thrombotic disorders, and cardiovascular conditions^[1].

References:

[1]. Mead TJ, et al. ADAMTS proteins in human disorders. Matrix Biol. 2018 Oct;71-72:225-239. [Content Brief]

ADAMTS Related Products (19)
Antibodies (7)

By Effects:	Inhibitors (16) Antagonist (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-137430

Aldumastat	Inhibitor	99.36%
Aldumastat (GLPG1972; S201086) is a potent, seletive and orally active ADAMTS-5 (IC₅₀=19 nM) inhibitor, and has 8-fold seletivity over ADAMTS-4 (IC₅₀=156 nM). Aldumastat has anticatabolic activity and is used for osteoarthritis research.

HY-114996

ADAMTS-5 Inhibitor	Inhibitor	99.59%
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).

HY-162284

BAY-9835	Antagonist	99.46%
BAY-9835, a chemical probe, is an orally active ADAMTS7 and ADAMTS12 antagonist with IC₅₀s of 6 nM and 30 nM, respectively. BAY-9835 exhibits inhibitory potencies vs mouse (mIC₅₀ = 8 nM) and rat (rIC₅₀ = 27 nM) ADAMTS7 enzymes. BAY-9835 is very selective against a range of off-targets and metalloproteases. BAY-9835 can be used for the study of atherogenesis.

HY-P10398

5-FAM-TEGEARGSVILLK(5-TAMRA)K-NH2 TFA
5-FAM-TEGEARGSVILLK(5-TAMRA)K-NH2 TFA is a substrate for ADAMTS-4/ADAMTS-5, and can be used to detect ADAMTS-4 or ADAMTS-5 activity.

HY-145061

ADAMTS-5-IN-3	Inhibitor	98.89%
ADAMTS-5-IN-3 (Example 37-2) is a potent inhibitor of ADAMTS-5 and ADAMTS-4 with IC₅₀s of 8 and 12 nM, respectively. ADAMTS-5-IN-3 can be used for the research of diseases involving degradation of cartilage or disruption of cartilage homeostasis, in particular osteoarthrosis and/or rheumatoid arthritis.

HY-P992336

CRB0017	Inhibitor
CRB0017 is a recombinant monoclonal antibody targeting ADAMTS5, with high affinity for the spacer domain of ADAMTS5 and strong antigen specificity. CRB0017 binds to the spacer domain of ADAMTS5 and reduces the proteolytic activity of this enzyme. CRB0017 delays articular cartilage degradation, alleviates the pathological severity of osteoarthritis, and decreases the osteoarthritis histopathological score. CRB0017 is applicable to the research of osteoarthritis.

HY-180781

ADAMTS-5-IN-4	Inhibitor
ADAMTS-5-IN-4 (Compound 4b) is a selective ADAMTS5 inhibitor with an IC₅₀ of 9.4 μM. ADAMTS-5-IN-4 significantly inhibits the degradation of Aggrecan in the implants of the osteoarthritis model. ADAMTS-5-IN-4 effectively inhibits the pseudopod elongation and directional migration of ovarian cancer cells. ADAMTS-5-IN-4 shows significant cytotoxicity to HEK293T cells, human chondrocytes, and porcine chondrocyte implants. ADAMTS-5-IN-4 can be used for the study of osteoarthritis and ovarian cancer.

HY-P992358

GSK2394002	Inhibitor
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.

HY-P99671

Isecarosmab	Inhibitor
Isecarosmab (M-6495) is an anti-ADAMTS monoclonal antibody (mAb) with a K_D value of 3.65 pM. Isecarosmab has chondroprotective and anti-inflammatory activities. Isecarosmab can bind albumin to extend plasma half-life.

HY-N4090

Vicenin 3	Inhibitor	99.90%
Vicenin 3 is an angiotensin-converting enzyme (ACE) inhibitor (IC₅₀ = 46.91 μM) that can be isolated from the aerial parts of Desmodium styracifolium. Vicenin 3 ameliorates IL-1β-induced extracellular matrix degradation in SW1353 chondrocytes by regulating the MAPK pathway. Vicenin 3 can be used for the study of osteoarthritis (OA) and hypertension.

HY-160822

AGG-523	Inhibitor	99.32%
AGG-523 (PF-5212371) is an orally active, reversible, non-hydroxamate, zinc-binding selective inhibitor of ADAMTS4 and ADAMTS5 with IC₅₀of <0.03 and 0.04 μM. AGG-523 also inhibits MMP-2, -8, 12 activity AGG-523 attenuates release of aggrecanase-generated ARG-aggrecan fragments into synovial fluid, reduces surgery-induced ARG-aggrecan release in rat joint models, and inhibits aggrecanase activity to slow cartilage degradation. AGG-523 can be used for the research of osteoarthritis.

HY-135710

ADAMTS-5-IN-2	Inhibitor	98.73%
ADAMTS-5-IN-2 is an inhibitor of ADAMTS-5 (IC₅₀: 9.6 μM) and BoNT/A LC (IC₅₀: 0.71 μM). ADAMTS-5-IN-2 can be used in research related to botulism, osteoarthritis, and other conditions.

HY-168003

ADAMTS7-IN-1	Inhibitor	98.91%
ADAMTS7-IN-1 (Compound 3a) is an effective and selective inhibitor of ADAMTS7 with a K_i value of 9 nM. ADAMTS7-IN-1 can be used in the research of atherosclerosis.

HY-P4003

Adamtsostatin 16	Inhibitor
Adamtsostatin 16 is an anti-angiogenic 17-amino acid peptide containing type I thrombospondin motifs.

HY-172394

ZSNI-21	Inhibitor
ZSNI-21 is a ADAM17/HDAC2 inhibitor with ADAM17 IC₅₀ 0.939 μM and HDAC2 IC₅₀ 0.844 μM. ZSNI-21 regulates the expression of apoptosis-related proteins (Bax, Bcl-2) and Cyclin D1, and induces apoptosis.. ZSNI-21 can be used for the research of hepatocellular carcinoma, breast cancer, and non-small cell lung cancer.

HY-P10468

5-FAM-TEGEARGSVILLK(5-TAMRA)K-NH2
5-FAM-TEGEARGSVILLK(5-TAMRA)K-NH2 is a substrate for ADAMTS-4/ADAMTS-5, and can be used to detect ADAMTS-4 or ADAMTS-5 activity.

HY-P4002

Adamtsostatin 18	Inhibitor
Adamtsostatin 18 is an anti-angiogenic peptide derived from proteins containing type I thrombospondin motifs. Adamtsostatin 18 inhibits cell migration and proliferation.

HY-P4001

Adamtsostatin 4	Inhibitor
Adamtsostatin 4 is an anti-angiogenic peptide. Adamtsostatin 4 can be used for the research of anti-angiogenic.

HY-153505

ADAMTS-4/5-IN-1	Inhibitor
ADAMTS-4/5-IN-1 is an orally active, and selective dual ADAMTS-4/5 inhibitor with IC₅₀ values of 2 nM for human ADAMTS-4 and human ADAMTS-5, respectively. ADAMTS-4/5-IN-1 exhibits high selectivity against MMP enzymes. ADAMTS-4/5-IN-1 reduces aggrecan degradation products in synovial fluid. ADAMTS-4/5-IN-1 can be used for the research of osteoarthritis.

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ADAMTS

ADAMTS Related Products (19)

Antibodies (7)

ADAMTS Related Products (19):