CXCR Inhibitor

ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a K_i of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC₅₀ of 2.9 μM.

Minecoside is a CXCR4/STAT3 inhibitor with anticancer and anti-inflammatory activity. Minecoside decreases CXCR4 expression and suppresses STAT3 activation, thus to inhibit CXCL 12-induced invasion. Minecoside potently inhibits cancer metastasis and promotes apoptotic progression.

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.

Pegevongitide (AV-001) is a Tie2 agonist. Pegevongitide resists the increased endothelial cell permeability induced by SARS-CoV-2 infection. Pegevongitide activates the angiogenin (angiogenin)/Tie2 signaling pathway. Pegevongitide reduces perivascular space dilation and upregulates perivascular Aquaporin-4 expression. Pegevongitide decreases the expression of TNF-α, PAI-1, CXCL9 and P-selectin, improves white matter integrity, enhances cognitive function and exerts neuroprotective effects. Pegevongitide improves white matter integrity in middle-aged rats with vascular dementia induced by multiple microinfarctions. Pegevongitide can be used in related research on diseases such as COVID-19 and vascular dementia.

CCR7 antagonist 1 (30c) is a dual CXCR2 (IC₅₀ of 11.02 μM) and CCR7 (IC₅₀ of 0.43 μM) antagonist.

Olopatadine (ALO4943A; KW4679) is an orally active histamine H1 receptor antagonist and mast cell stabilizer. Olopatadine exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine also reduces the expression levels of CXCR3 on the surface of CD4⁺ and CD8⁺ T cells. Olopatadine inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis.

CCX662 is a selective CXCR7 inhibitor with human IC₅₀ values of 9 nM (buffer) and 18 nM (100% human serum), and rat IC₅₀ of 14 nM (100% rat serum). CCX662 blocks CXCL12 binding to CXCR7, inhibits CXCR4-directed trans-endothelial migration of CXCR4⁺/CXCR7⁺ cells. CCX662 can be used for the research of glioblastoma multiforme.

CXCR4-IN-3 (compound XVI) is an orally active and potent inhibitor targeting the inflammation-related receptor CXCR4, with an IC₅₀ of 3.2 nM. CXCR4-IN-3 exhibits potent antichemotactic activity, at 79.19±2.33% inhibition. CXCR4-IN-3 shows anti-inflammatory activity. CXCR4-IN-3 can be used for IBD (inflammatory bowel disease) research.

Anti-Mouse/Human CXCL12 Antibody (K15C) is an antibody targeting SDF-1/CXCL12. Anti-Mouse/Human CXCL12 Antibody (K15C) blocks the biological activity of SDF-1 secreted by cancer-associated fibroblasts. Anti-Mouse/Human CXCL12 Antibody (K15C) inhibits tumor growth, reduces tumor microvessel density, and decreases the proportion of Sca1⁺CD31⁺ endothelial progenitor cells in tumors. Anti-Mouse/Human CXCL12 Antibody (K15C) can be used for research on aggressive human breast cancer. The recommended isotype control is Mouse IgG2a kappa, Isotype Control (HY-P99978).

pCXCL8-1aa is an anti-inflammatory peptide. pCXCL8-1aa competitively inhibits the binding of CXCL8 to glycosaminoglycans such as heparin sulfate (HS) by binding with high affinity. This reduces the presentation of CXCL8 on the surface of vascular endothelial cells, thereby inhibiting neutrophil migration and inflammatory responses. pCXCL8-1aa can be used to study inflammatory diseases such as rheumatoid arthritis.

Snail IN-1 is an orally active Snail inhibitor with a Ka of 0.36 μM.Snail IN-1 disrupts Snail-CBP interaction, accelerates Snail protein degradation, reduces Snail acetylation, increases Snail polyubiquitination, and selectively downregulates Snail protein without altering other EMT transcription factors.Snail IN-1 reduces atherosclerotic plaque burden, modulates inflammation and plaque stability factors, downregulates CCL5, CXCL10, MMP2, and MMP9, and upregulates α-smooth muscle actin.Snail IN-1 exerts anti-inflammatory and plaque-stabilizing properties.Snail IN-1 can be used for the research of atherosclerosis.

Anti-Mouse CXCL16 Antibody (12-81) is an antibody targeting mouse CXCL16. Anti-Mouse CXCL16 Antibody (12-81) blocks the CXCL16/CXCR6 signaling axis. Anti-Mouse CXCL16 Antibody (12-81) reduces the recruitment of CD8⁺ T cells into the brain. Anti-Mouse CXCL16 Antibody (12-81) alleviates the reduction of hippocampal neurogenesis. Anti-Mouse CXCL16 Antibody (12-81) attenuates anxiety-like behaviors in mice. Anti-Mouse CXCL16 Antibody (12-81) can be used in studies related to anxiety-like behaviors. The recommended isotype control is Rat IgG1 kappa, Isotype Control (HY-P99979).

YU241279 is an orally active CXCR5 inhibitor. YU241279 inhibits CXCL13-mediated Gαq-dependent calcium influx and Gαi2-dependent cAMP reduction in CXCR5-expressing cells. YU241279 inhibits the proliferation of CXCR5-expressing lymphoma cells. YU241279 reduces tumor burden in the peripheral blood and bone marrow of mice implanted with lymphoma tissues. YU241279 is well tolerated during oral administration in mice, maintains stable plasma drug concentrations, and shows no metabolic changes. YU241279 can be used in the research of angioimmunoblastic T-cell lymphoma and Burkitt B-cell lymphoma.

CXCR3 Human Pre-designed siRNA Set A contains three designed siRNAs for CXCR3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Anti-Mouse CCL5 Antibody (R6G9) is a neutralizing agent that binds to CCL5 to inhibit its chemotactic activity towards CD4⁺ T cells.Anti-Mouse CCL5 Antibody (R6G9) does not suppress CD4⁺ T cell migration towards infection-derived liver cells, reduce CD4⁺ T cell hepatic accumulation, or impair CD4⁺ T cell migratory capacity.Anti-Mouse CCL5 Antibody (R6G9) serves as a tool to assess CCL5’s role in in vivo target cell killing by LCMV-specific CD8⁺ effector T cells.Anti-Mouse CCL5 Antibody (R6G9) can be used for the research of malaria infection and lymphocytic choriomeningitis virus infection.

CXCR2 Human Pre-designed siRNA Set A contains three designed siRNAs for CXCR2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CXCR4 antagonist 10 (compound 21) is a potent antagonist of CXCR4, with the IC₅₀ of 7.8 nM. CXCR4 antagonist 10 plays an important role in cancer research.

Hit 14 is an inhibitor for C-X-C chemokine receptor type 4 (CXCR4) with IC₅₀ of 254 nM. Hit 14 inhibits the migration and invasion of cell MDA-MB-231. Hit 14 inhibits the Akt phosphorylation, exhibits anti-inflammatory activity, and ameliorateds the ear swelling and damage in mouse models.

ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a K_i of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC₅₀ of 2.9 μM.

vMIP-II (1-21) (NT21MP) TFA is an inhibitor of CXCR4. vMIP-II (1-21) TFA interacts broadly with CC and CXC chemokine receptors. vMIP-II (1-21) TFA inhibits CXCR4 by competing with 125I-SDF-1R for binding sites (IC₅₀=190 nM).