8 Results for "

Aggrecan Inhibitors

" in MedChemExpress (MCE) Product Catalog:
Products (8)

8 Results for "Aggrecan Inhibitors" in MCE Product Catalog:

Cat. No.: HY-160822
CAS No.: 920289-29-8
Synonyms: PF-5212371
Target:  

ADAMTS MMP

Research Areas:  

Inflammation/Immunology

AGG-523 (PF-5212371) is an orally active, reversible, non-hydroxamate, zinc-binding selective inhibitor of ADAMTS4 and ADAMTS5 with IC50 of <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 .
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Cat. No.: HY-P5542
CAS No.: 1251838-01-3
Synonyms: SB-01; Peniel 2000
Target:  

Factor Xa TGF-beta/Smad

Research Areas:  

Inflammation/Immunology

Vicatertide (SB-01, Peniel 2000) is a polypeptide with both competitive inhibitory activity against TGF-β1 and selective inhibitory activity against human factor XIa (hFXIa, with a Ka of 80 nM for hFXIa). Vicatertide binds allosterically to the two binding sites of dimeric hFXI/hFXIa, while directly binding to activated TGF-β1, selectively blocking the Smad1/5/8 pathway and maintaining low-level activation of the Smad2 pathway to enhance the synthesis of type Ⅱ collagen and aggrecan. Vicatertide inhibits thrombus formation in arteriovenous thrombosis models, and also reduces thrombus weight and thrombus incidence in mouse lung cancer models. Vicatertide can be used for research on degenerative disc disease and thrombosis-related diseases .
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Cat. No.: HY-N6812
CAS No.: 39089-30-0
Karacoline is an orally active PPARγ activator and ERK/JNK MAPK inhibitor. Karacoline restricts ROS production, maintains mitochondrial membrane potential, and inhibits pulmonary cell apoptosis. Karacoline inhibits NF-κB pathway activation, reduces acetylation levels of p65 and the expression of MMP14 and MMP9, enhances the expression of type II collagen (collagen II) and aggrecan (aggrecan), and suppresses extracellular matrix degradation. In a mouse model of sepsis-induced acute lung injury, Karacoline alleviates lung injury, inhibits the release of IL-1β, IL-6 and TNF-α, increases the Bcl-2/BAX ratio, and reduces caspase 3 expression. Karacoline can be used in research related to acute lung injury and intervertebral disc degeneration .
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Cat. No.: HY-P10462
CAS No.: 1403753-45-6
Synonyms: Synthetic anti-inflammatory peptide 15
Target:  

HDAC NF-κB

Research Areas:  

Inflammation/Immunology

SAP15 (Synthetic anti-inflammatory peptide 15) is a synthetic anti-inflammatory peptide consisting of 15 amino acids designed from human beta-defensin 3. SAP15 has the ability to penetrate cells and is able to induce downregulation of intracellular inflammation. SAP15 inhibits inflammation by inhibiting the phosphorylation of HDAC5 and thereby reducing the phosphorylation of NF-κB p65. SAP15 inhibits HDAC5 and NF-κB p65 phosphorylation in LPS (HY-D1056)-induced macrophages. SAP15 increases the expression of aggrecan and type II collagen and decreases the expression of osteocalcin in LPS-induced chondrocytes. SAP15 can be used in the study of inflammation regulation and anti-inflammatory therapy of biomaterials .
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Cat. No.: HY-P10462A
Synonyms: Synthetic anti-inflammatory peptide 15 acetate
Target:  

HDAC NF-κB

Research Areas:  

Inflammation/Immunology

SAP15 (Synthetic anti-inflammatory peptide 15) acetate is a synthetic anti-inflammatory peptide consisting of 15 amino acids designed from human beta-defensin 3. SAP15 acetate has the ability to penetrate cells and is able to induce downregulation of intracellular inflammation. SAP15 acetate inhibits inflammation by inhibiting the phosphorylation of HDAC5 and thereby reducing the phosphorylation of NF-κB p65. SAP15 acetate inhibits HDAC5 and NF-κB p65 phosphorylation in LPS (HY-D1056)-induced macrophages. SAP15 acetate increases the expression of aggrecan and type II collagen and decreases the expression of osteocalcin in LPS-induced chondrocytes. SAP15 acetate can be used in the study of inflammation regulation and anti-inflammatory therapy of biomaterials .
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Cat. No.: HY-P992358

Target:  

ADAMTS

Research Areas:  

Cardiovascular Disease

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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Cat. No.: HY-153505
CAS No.: 1607004-34-1
Target:  

ADAMTS

Research Areas:  

Inflammation/Immunology

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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Cat. No.: HY-180781
Target:  

ADAMTS

Research Areas:  

Inflammation/Immunology Cancer

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 .
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