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CXCR2 Inhibitors

" in MedChemExpress (MCE) Product Catalog:

28

Inhibitors & Agonists

1

Peptides

1

Inhibitory Antibodies

1

Natural
Products

Targets Recommended:
Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-16711
    SB225002
    55+ Cited Publications

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM.
    SB225002
  • HY-15251
    Reparixin
    Maximum Cited Publications
    62 Publications Verification

    Repertaxin; DF 1681Y

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    Reparixin
  • HY-119339
    SX-682
    5+ Cited Publications

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity .
    SX-682
  • HY-120878
    CXCR2-IN-2
    1 Publications Verification

    		 CXCR Inflammation/Immunology
    CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM .
    CXCR2-IN-2
  • HY-153450
    JBI-589

    		Protein Arginine Deiminase Cancer
    JBI-589 is a non-covalent PAD4 isoform-selective inhibitor with oral bioavailability. JBI-589 reduces CXCR2 expression and blocks neutrophil chemotaxis. JBI-589 reduces primary tumor and metastases, and enhances the anti-tumor effect of checkpoint inhibitors. JBI-589 can be used in cancer research .
    JBI-589
  • HY-165428
    SCH-900875

    		CXCR Arrestin Inflammation/Immunology
    SCH-900875 is an orally active, brain-penetrant and selective CXCR3 receptor inhibitor, which also shows high selectivity over CXCR1 and CXCR2 receptors. SCH-900875 binds to CXCR3, blocking the binding of ligands CXCL9, CXCL10, and CXCL11, inhibiting downstream G protein and β-arrestin signaling pathways to suppress inflammatory cell migration. SCH-900875 is promising for research of autoimmune diseases (rheumatoid arthritis, multiple sclerosis) and inflammatory disorders (psoriasis, inflammatory bowel disease) .
    SCH-900875
  • HY-120427
    Cosalane
    1 Publications Verification

    NSC 658586

    		 CCR CXCR HIV HSV Infection Inflammation/Immunology
    Cosalane (NSC 658586) is a CCR7 (IC50 = 2.43 μM) and CXCR2 antagonist (IC50 = 0.66 μM). Cosalane is an inhibitor of HIV replication with a wide range of activity against HIV-1 isolates, HIV-2, Rauscher murine leukemia virus, HSV-1, HSV-2 and human cytomegalovirus. Cosalane inhibits both attachment of gp120 to CD4. Cosalane inhibits human and murine CCR7 in response to both CCL19 and CCL21 agonists. Cosalane can be studied in research for HIV or attenuating acute graft-versus-host disease (aGVHD) in allogeneic hematopoietic stem cell transplantation (HSCT) .
    Cosalane
  • HY-12927
    SX-517

    		CXCR Inflammation/Immunology
    SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .
    SX-517
  • HY-16981
    SB-332235

    		CXCR Inflammation/Immunology
    SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells .
    SB-332235
  • HY-18263C
    Elubrixin tosylate

    SB-656933 tosylate

    		 CXCR Interleukin Related Inflammation/Immunology
    Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
    Elubrixin tosylate
  • HY-P4846
    Ac-Pro-Gly-Pro-OH
    2 Publications Verification

    		 CXCR Apoptosis IFNAR TNF Receptor Interleukin Related Infection Inflammation/Immunology
    Ac-Pro-Gly-Pro-OH is an endogenous degradation product of extracellular collagen and acts as a CXCR2 agonist . Ac-Pro-Gly-Pro-OH exerts bactericidal activity by generating hydrogen peroxide, inhibits pulmonary inflammation, and reduces immune cell apoptosis (apoptosis). Ac-Pro-Gly-Pro-OH promotes the production of IFN-γ and inhibits the production of TNF-α and IL-6 in leukocytes. Ac-Pro-Gly-Pro-OH increases the survival rate of mice in sepsis models, enhances the bactericidal activity of neutrophils, acts as a neutrophil chemoattractant, induces neutrophil polarization, and regulates inflammatory and repair processes. Ac-Pro-Gly-Pro-OH induces chronic inflammation and tissue remodeling through sustained action. Ac-Pro-Gly-Pro-OH is released via alkaline hydrolysis of corneal proteins in alkali-injured eyes, thereby driving the early infiltration of neutrophils into the cornea. Ac-Pro-Gly-Pro-OH is applicable to research related to sepsis, chronic obstructive pulmonary disease, cystic fibrosis, bronchiolitis obliterans syndrome, severe asthma, idiopathic pulmonary fibrosis, and corneal ulcer .
    Ac-Pro-Gly-Pro-OH
  • HY-15251A
    (Rac)-Reparixin

    (Rac)-Repertaxin; (Rac)-DF 1681Y

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    (Rac)-Reparixin is the isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    (Rac)-Reparixin
  • HY-N2573
    Corydalmine

    L-Corydalmine; TLZ-16

    		 Fungal CXCR Infection Neurological Disease
    Corydalmine (L-Corydalmine) inhibits spore germination of some plant pathogenic as well as saprophytic fungi . Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity . Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway .
    Corydalmine
  • HY-163475
    CXCL-CXCR1/2-IN-1
    1 Publications Verification

    		 CXCR Cancer
    CXCL-CXCR1/2-IN-1 is an orally active ELR +CXCL-CXCR1/2 pathway inhibitor with an EC50 of 42.7 nM for CXCR2 . CXCL-CXCR1/2-IN-1 shows anticancer and antiangiogenic effects .
    CXCL-CXCR1/2-IN-1
  • HY-179387
    CXCR2-IN-3

    		CXCR Autophagy NOD-like Receptor (NLR) Reactive Oxygen Species (ROS) Apoptosis Cancer
    CXCR2-IN-3 is a CXCR2 inhibitor with an IC50 of 11.37 μM. CXCR2-IN-3 mediates CXCR2-Ca 2+ signalling inhibition halted autophagic flux, subsequently facilitating ROS-mediated apoptotic cell death. CXCR2-IN-3 suppresses the CXCR2-NLRP3 canonical pathway, suppressing pre-tumorigenic markers. CXCR2-IN-3 causes autophagy-dependent cell death in polyploid giant cancer cells (PGCCs). CXCR2-IN-3 can be used for the research of oral squamous cell carcinoma (OSCC) .
    CXCR2-IN-3
  • HY-18263A
    Elubrixin

    SB-656933

    		 CXCR Interleukin Related Inflammation/Immunology
    Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
    Elubrixin
  • HY-124056
    AZ10397767

    		CXCR Cancer
    AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC50 of 1 nM. AZ10397767 attenuates the Oxaliplatin (HY-17371)-induced NF-κB transcriptional activity and potentiates Oxaliplatin-induced apoptosis in androgen-independent prostate cancer (AIPC) cells. AZ10397767 significantly inhibits neutrophil recruitment into tumors which then adversely affects tumor growth in vitro and in vivo .
    AZ10397767
  • HY-162505
    SQA1

    		CCR CXCR Inflammation/Immunology Cancer
    SQA1, a squaramide (SQA) derivative, is a CCR6 antagonist with a Kd of 250 nM. SQA1 is also a CXCR2 inhibitor. The intracellular pocket occupied by SQA1 overlaps with the G protein binding site and stabilizes the closed conformation of the intracellular pocket .
    SQA1
  • HY-144780
    CXCR2 antagonist 4

    		CXCR Cancer
    CXCR2 antagonist 4 (compound 7) is a potent CXCR2 antagonist with an IC50 value of 0.13 μM. CXCR2 antagonist 4 can inhibit CXCL8-induced cytosolic calcium increase (IC50 = 27 μM). CXCR2 antagonist 4 can be used for researching anticancer .
    CXCR2 antagonist 4
  • HY-119234
    CX4338

    		CXCR Inflammation/Immunology
    CX4338 is a CXCL8-mediated chemokine inhibitor with the activity of inhibiting CXCR2-mediated cell migration. CX4338 selectively inhibits CXCR2-mediated β-arrestin-2 recruitment and receptor internalization while enhancing CXCR2-mediated MAPK activation. CX4338 also inhibited CXCL8-induced chemotaxis, showing efficacy in CXCR2-overexpressing cells and human neutrophils. In vivo, CX4338 significantly reduced LPS-induced neutrophil numbers in mouse bronchoalveolar lavage fluid. The mechanism of action of CX4338 is to selectively inhibit CXCR2-mediated β-arrestin-2 activation, which is sufficient to inhibit CXCL8-mediated chemotaxis .
    CX4338
  • HY-15251R
    Reparixin (Standard)

    Repertaxin (Standard); DF 1681Y (Standard)

    		 CXCR Reference Standards Inflammation/Immunology Endocrinology Cancer
    Reparixin (Standard) is the analytical standard of Reparixin. This product is intended for research and analytical applications. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    Reparixin (Standard)
  • HY-N2573A
    Corydalmine hydrochloride

    L-Corydalmine hydrochloride; TLZ-16-CL

    		 Fungal CXCR Infection Neurological Disease
    Corydalmine hydrochloride inhibits spore germination of some plant pathogenic as well as saprophytic fungi . Corydalmine hydrochloride acts as an oral analgesic agent, exhibiting potent analgesic activity . Corydalmine hydrochloride alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway .
    Corydalmine hydrochloride
  • HY-18263
    Elubrixin hydrochloride

    SB-656933 hydrochloride

    		 CXCR Interleukin Related Inflammation/Immunology
    Elubrixin (SB-656933) hydrochloride is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin hydrochloride inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin hydrochloride has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
    Elubrixin hydrochloride
  • HY-18263CR
    Elubrixin tosylate (Standard)

    SB-656933 tosylate (Standard)

    		 CXCR Interleukin Related Reference Standards Inflammation/Immunology
    Elubrixin (tosylate) (Standard) is the analytical standard of Elubrixin (tosylate). This product is intended for research and analytical applications. Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
    Elubrixin tosylate (Standard)
  • HY-110268
    NVP CXCR2 20

    		CXCR Inflammation/Immunology
    NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD) .
    NVP CXCR2 20
  • HY-124183
    SX-576

    		CXCR Inflammation/Immunology
    SX-576 is a CXCR1 and CXCR2 antagonist with IC50 values of 31 nM and 21 nM, respectively. SX-576 inhibits neutrophil infiltration in a rat model of pulmonary inflammation. SX-576 can be used in studies related to pulmonary inflammation .
    SX-576
  • HY-15251AR
    (Rac)-Reparixin (Standard)

    (Rac)-Repertaxin (Standard); (Rac)-DF 1681Y (Standard)

    		 CXCR Reference Standards Inflammation/Immunology Endocrinology Cancer
    (Rac)-Reparixin (Standard) is the analytical standard of (Rac)-Reparixin. This product is intended for research and analytical applications. (Rac)-Reparixin is the isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
    (Rac)-Reparixin (Standard)
  • HY-P992035
    AMY109

    		Interleukin Related Endocrinology
    AMY109 is an anti-human interleukin-8 (IL-8) monoclonal antibody, with a Ka of 36.8 pM for human IL-8, and a Ka of 380 pM for cynomolgus monkey IL-8. AMY109 binds to human and cynomolgus monkey IL-8 in a pH-dependent manner, inhibits IL-8-mediated activation of CXCR1 and CXCR2, and blocks the downstream biological activities of IL-8. AMY109 inhibits neutrophil recruitment to endometriotic lesions and suppresses monocyte chemoattractant protein-1 production by neutrophils. AMY109 is applicable to research related to endometriosis .
    AMY109

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