61

61 Publications Verification

Target:

Research Areas:

Cardiovascular Disease Inflammation/Immunology

GSK484 is a PAD4 inhibitor that effectively inhibits protein citrullination and the formation of neutrophil extracellular traps (NETs) by blocking the catalytic activity of PAD4. GSK484 suppresses the production of histone H3, MHC-I expression, CD8 ⁺ T cell activation, proliferation and inflammatory cytokine release. GSK484 reduces inflammation and bone destruction in collagen-induced rheumatoid arthritis, alleviates pain and mast cell activation in sickle cell disease, and improves myocardial ischemia-reperfusion injury and experimental colitis. In addition, GSK484 restores intestinal microbial homeostasis by reversing ferroptosis-induced dysbiosis. GSK484 can be used to study the disease mechanisms of rheumatoid arthritis, sickle cell disease, thrombosis, myocardial injury, colitis and other conditions .

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4

Bexobrutideg

4 Cited Publications

Cat. No.: HY-153321

CAS No.: 2649400-34-8

Purity: 98.67%

Synonyms: NX-5948; BTK-IN-24

Target:

PROTACs Btk

Research Areas:

Inflammation/Immunology

Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .

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3

Caerulomycin A

3 Cited Publications

Cat. No.: HY-114495

CAS No.: 21802-37-9

Purity: ≥98.0%

Synonyms: Cerulomycin; Caerulomycin

Category:

Microorganisms Anti-inflammation/Immunoregulatory Antibiotics Disease Research Antibacterial Anticancer Disease Research Fields Inflammation/Immunology Other Antibiotics

Target:

Fungal Antibiotic

Caerulomycin A is an orally active immunomodulator and antimicrobial agent. Caerulomycin A targets Smad3, STAT1 and GATA-3. Caerulomycin A downregulates GATA-3 expression, inhibits Th2 cell differentiation and Th2 cytokine production, reduces IgE levels, and alleviates pulmonary inflammatory responses and eosinophil infiltration. Caerulomycin A ameliorates collagen-induced arthritis symptoms, reduces joint inflammation and synovitis, and decreases the levels of proinflammatory cytokines in joints. Caerulomycin A inhibits the growth of some filamentous fungi, yeasts and specific bacteria. Caerulomycin A can be used in research related to arthritis and asthma .

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2

ACT017

2 Cited Publications

Cat. No.: HY-P99644

CAS No.: 2101829-58-5

ACT017 is a Fab fragment of humanized anti-GPVI monoclonal antibody. ACT017 inhibits collagen-induced platelet aggregation. ACT017 has the potential for the research of acute ischemic stroke .

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2

TMI-1

2 Cited Publications

Cat. No.: HY-101448

CAS No.: 287403-39-8

Purity: 99.59%

Synonyms: WAY-171318

Target:

MMP Apoptosis Interleukin Related TNF Receptor Caspase

Research Areas:

Infection Neurological Disease Inflammation/Immunology Cancer

TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC₅₀ of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions .

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2

(S)-S007-1558

2 Cited Publications

Cat. No.: HY-144390

CAS No.: 1327156-14-8

Purity: 99.78%

Synonyms: GPVI antagonist 1

Target:

Glycoprotein VI

Research Areas:

Cardiovascular Disease

(S)-S007-1558 (compound 5) is a glycoprotein VI (GPVI) platelet receptor antagonist. (S)-S007-1558 inhibits collagen-induced platelet aggregation with an IC₅₀ of 25.3 μM .

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1

VU6015929

1 Cited Publications

Cat. No.: HY-135401

CAS No.: 2442597-56-8

Purity: 99.50%

Target:

Discoidin Domain Receptor

Research Areas:

Inflammation/Immunology

VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC₅₀s of 4.67 nM and 7.39 nM, respectively. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production .

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1

L-161982

1 Cited Publications

Cat. No.: HY-108559

CAS No.: 147776-06-5

Purity: 99.30%

Target:

Prostaglandin Receptor

Research Areas:

Inflammation/Immunology

L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice .

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1

SP-100030

1 Cited Publications

Cat. No.: HY-110177

CAS No.: 154563-54-9

Purity: 99.57%

Target:

NF-κB

Research Areas:

Inflammation/Immunology

SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC₅₀s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA) .

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