SCH 546738 is a novel, potent and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
SDF-1α (human) is a mononuclear cells chemoattractant that can bind to CXCR4. SDF-1α plays a central role in stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis and ventricular remodelling following myocardial infarction. SDF-1α (human) can be used in cardiovascular disease research[1][2].
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[1][2].
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[1][2][3].
vMIP-II (1-21) is a CXCR4 antagonist. vMIP-II has broad-spectrum interaction with CC and CXC chemokine receptors. vMIP-II (1-21) binds with CXCR4 with an IC50 value of 190 nM for competing with CXCR4 binding of 125I-SDF-1R[1].
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2].
Elubrixin is a interleukin 8 inhibitor and CXCR2 selective antagonist.
Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
AZD-8309 (AZD8309) is a potent and orally bioavailable CXCR2 antagonist that has been proposed to regulate the transmigration of neutrophils; significantly reduces MPO in the pancreas and lungs, and reduces intrapancreatic trypsin and elastase activity in caerulein-pancreatitis; also reduces cathepsin B activity and MPO in taurocholate-pancreatitis; also antagonises the CCR2b receptor but it is 10-fold less potent than at CXCR2. COPD Phase 1 Clinical
A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM; prevents PMN infiltration and tissue damage in several models of IR injury in vivo; abrogates motility and induces apoptosis in cultured cutaneous and uveal melanoma cells and xenografts; also prevents inflammation-mediated damage in MLD-STZ, prevents and reverses diabetes in NOD mice. Diabetes Phase 2 Clinical
CXCR4 antagonist 2 is a CXCR4 antagonist with an IC50 value of 47 nM.
AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM[1][2][3].
ACT-672125 is a potent CXCR3 antagonist with IC50 value of 239 nM in human blood. ACT-672125 has activity for hERG with IC50 value of 18μM. ACT-672125 can be used for the research of autoimmune diseases[1].
A potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively; inhibits CXCL1-induced Ca(2+) flux in human PMNs but has no effect on the Ca(2+) flux induced by C5a, fMLF, or PAF; antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation in recombinant HEK293 cells expressed CXCR2; significantly inhibits inflammation in an in vivo murine model (0.2 mg/kg iv).
Pentixafor is a peptide that targets CXCR4. Pentixafor is capable of being labelled with 68Gallium (68Ga) for positron emission tomography (PET) imaging[1].
Danirixin is a selective, and reversible CXCR2 antagonist, with IC50 of 12.5 nM for CXCL8.
TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
VUF11207 fumarate (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7[1].
AMD-070 is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
ATI-2341 is a CXCR4 agonist, induces CXCR4-dependent calcium flux, with an EC50 of 194 nM in CCRF-CEM cells. ATI-2341 is also a potent and efficacious mobilizer of bone marrow hematopoietic cells[1].
CXCR4 antagonist 9 (Compound 2) is a CXCR4 antagonist with an IC50 of 15 nM. CXCR4 antagonist 9 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 1.3 nM[1].
Eldelumab (BMS-936557) is a humanised 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[1][2].
USL311 is a selective CXCR4 antagonist, with anti-tumor activity[1].
CXCR7 antagonist-1 is an inhibitor of the binding of the SDF-1 chemokine (CXCL12 chemokine) or I-TAC (CXCL11) to the chemokine receptor CXCR. CXCR7 antagonist-1 prevents tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128)[1].
CXCR4 antagonist 7 (Compound PARA-B) is a CXCR4 antagonist with the IC50 of 9.3 nM. CXCR4 antagonist 7 can be used for the research of HIV infection, inflammatory diseases, cancer, and WHIM syndrome[1].
ML339 is a potent and selective CXCR6 (IC50 of 140 nM) antagonist that is selective (IC50 >79 μM) against CXCR5, CXCR4, CCR6 and Apelin receptor (APJ). ML339 holds potential to advance the field of prostate cancer research[1].
CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator with an EC50 value of 100 nM. CXCR4 modulator-1 can be used for researching anti-inflammatory, anticancer and anti-HIV[1].
CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy with an IC50 value of 95 nM.