CXCR Inhibitor

AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC₅₀s of 8.0 and 8.2 nM, respectively.

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.

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.

Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC₅₀s of 1 and 100 nM, respectively.

Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.

LY2510924 is a potent and selective CXCR4 antagonist that blocks SDF-1 binding to CXCR4 with an IC₅₀ of 0.079 nM.

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.

Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.

Baminercept (BG 9924; TT-47) is an Ig fusion protein targeting the lymphotoxin β receptor (LTβR). Baminercept effectively regulates subsets of circulating immune cells by inhibiting LIGHT, LT-α1β2 and their receptors. Baminercept also increases blood lymphocyte counts and reduces plasma CXCL13 levels. Baminercept carries a high risk of hepatotoxicity. Baminercept can be used in research on rheumatoid arthritis and primary Sjögren's syndrome.

Anti-Mouse CXCR3/CD183 Antibody (CXCR3-173) is an anti-mouse CXCR3/CD183 IgG monoclonal antibody. Anti-Mouse CXCR3/CD183 Antibody (CXCR3-173) weakens the immune response by reducing the infiltration of CD4⁺ and CD8⁺ T cells. Anti-Mouse CXCR3/CD183 Antibody (CXCR3-173) significantly prolongs the survival time of heart or islet transplants in mice. Anti-Mouse CXCR3/CD183 Antibody (CXCR3-173) can be used for researches on immunology and cancer such as pancreatic cancer.

Eldelumab (BMS-936557) is a human anti-CXCL10 (IP-10) monoclonal antibody (IgG1 type). Eldelumab selectively binds to CXCL10 and blocks CXCL10-induced calcium flux and cell migration. Eldelumab can be used in studies of autoimmune and auto-inflammatory diseases such as rheumatoid arthritis, ulcerative colitis and crohn's disease.

Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) is an anti-mouse CXCL9/MIG IgG monoclonal antibody. Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) can reduce tumor infiltration of CD8⁺ cytotoxic T cells (CTLs). Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) can prolong the survival of transplanted hearts. Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) can be used for researches on immunology and cancer such as prostate cancer.

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

GSK699 is a KAT2A/B/PCAF/GCN5 PROTAC degrader. GSK699 induces proteasome-dependent degradation of KAT2A, KAT2B, PCAF and GCN5, regulates the histone acetyltransferase activity of the SAGA complex, and reduces the level of histone H3K9ac. GSK699 inhibits the growth of neuroblastoma, acute myeloid leukemia and small cell lung cancer cells. GSK699 reduces the production of inflammatory cytokines and chemokines, and impairs LPS-stimulated immune cell responses. GSK699 is applicable to research related to acute myeloid leukemia, small cell lung cancer, neuroblastoma and inflammatory diseases.

TFAM activator 1 is a TFAM activator. TFAM activator 1 increases TFAM protein levels, promotes mitochondrial DNA stability, increases mitochondrial DNA copy number, and prevents mitochondrial DNA from escaping into the cytoplasm. TFAM activator 1 improves cellular energy metabolism in cybrid cells. TFAM activator 1 reduces fibrosis markers in fibroblasts. TFAM activator 1 can be used in the research of mitochondrial encephalomyopathy, lactic acidosis, and stroke-like episodes syndrome, systemic sclerosis, and autoimmune diseases.

Quetmolimab (E6011) is a humanized anti-Fractalkine (CX3CL1) monoclonal antibody. Quetmolimab binds to membrane-bound and soluble Fractalkine, neutralizes Fractalkine-induced migration of CX3CR1-expressing cells, mediates target-bound complex elimination from serum. Quetmolimab suppresses free soluble Fractalkine levels in cynomolgus monkeys, with target engagement linked to increased serum total Fractalkine concentration. Quetmolimab can be used for the research of Crohn’s disease, rheumatoid arthritis, and primary biliary cholangitis.

Anti-Mouse CXCL10 Antibody (1F11) is a mouse CXCL10 antibody. Anti-Mouse CXCL10 Antibody (1F11) blocks the activity of CXCL10 and inhibits GPCR-dependent interstitial motility of Th1 cells in inflamed dermis. Anti-Mouse CXCL10 Antibody (1F11) can be used for research on inflammation-related diseases. Recommended isotype control: Polyclonal Armenian hamster IgG, Isotype Control (HY-P990305).

Olaptesed pegol (NOX-A12) sodium is a L-oligoribonucleotide aptamer targeting CXCL12 based on a pegylated structure. Olaptesed pegol sodium neutralizes CXCL12, and CXCL12 inhibition mobilizes chronic lymphocytic leukemia cells into the circulation and prevents their homing into the protective microenvironment. Olaptesed pegol sodium can enhances the infiltration of human primary T cells and NK cells and inhibit tumor growth companied with anti-PD-1 antibody. Olaptesed pegol sodium can be used for researches of colon cancer and lymphocytic leukemia.

CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonist with a pIC₅₀ of 9.3.

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).