CXCR

SX-682 is a potent, selective and orally bioavailable inhibitor of CXCR1/2 ,has the potential to treat castration-resistant prostate cancer.

Artemotil (SM-227) is a new, fast-acting antimalarial drug.

ALX 40-4C acetate is a CXCR4 inhibitor of the chemokine receptor (Ki = 1 μM) and suppresses the replication of X4 strains of HIV-1. ALX 40-4C acetate is an antagonist of the APJ receptor (IC50 = 2.9 μM).

NUCC-390, a novel small-molecule CXCR4 receptor agonist, selectively induces CXCR4 receptor internalization while acting antagonistically to AMD3100. This compound facilitates nerve functional recovery following neurodegeneration in vivo.

AMD-070 hydrochloride is a CXCR4 antagonist, is useful for Anti HIV.

rac-NBI-74330 is an effective and selective CXCR3 antagonist.

Elubrixin (SB-656933) inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation. Elubrixin is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist.

ATI-2341 acetate is an effective allosteric agonist of CXCR4, it activates Gα1 instead of Gα13. ATI-2341 acetate activates inhibitory heterotrimeric G protein (GI) to promote the inhibition of cAMP production and induce calcium mobilization.

Ac-Pro-Gly-Pro-OH is an acetyl-modified tripeptide compound that acts as a CXCR2 agonist.Ac-Pro-Gly-Pro-OH exhibits bactericidal and anti-inflammatory activity, inhibits apoptosis of immune cells, and suppresses the production of pro-inflammatory cytokines.Ac-Pro-Gly-Pro-OH has been used in the study of sepsis and inflammation in the lungs.

CTCE 9908 acetate is an antagonist of CXCR4 and inhibits migration in CXCR4-expressing ovarian cancer cells.

Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) is an antagonist of CXCR4 with IC50 of ～1 nM. It induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.

Ly2510924 acetate is an potent and selective CXCR4 antagonist. It prevents the binding of SDF-1 to CXCR4 with an IC50 of 0.079 nM.

TC14012 acetate is a serum-stable derivative of T140 which is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is also a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-cancer activity and anti-HIV activity.

AZD8309 is a potent, orally available antagonist of the chemokine receptor CXCR2 that regulates neutrophil transport, significantly reduces MPO in the pancreas and lung, and decreases trypsin and elastase activity in the pancreas.AZD8309 can be used to study a range of inflammatory diseases.

CXCR2-IN-1 has a pIC50 of 9.3 and is a CXCR2 antagonist of the central nervous system penetration agent.

Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent CXCR4 antagonist and an anti-angiogenic drug that is of potential value in treating choroid neovascularization.

SB225002 is a potent and selective CXCR2 antagonist inhibiting interleukin IL-8 binding to CXCR2.

Mogamulizumab (KW-0761) is a monoclonal antibody against T cell CC chemokine receptor 4. Mogamulizumab has anticancer activity, eliminating tumor cells through antibody dependent cytotoxicity (ADCC), and can be used to study cancer, adult T-cell leukemia/lymphoma (ATLL), cutaneous T-cell lymphoma (CTCL).

FC131 TFA (606968-52-9 free base) (FC131 TFA) is an antagonist of CXCR4 that inhibits the binding of [125I] -sdf-1 to CXCR4(IC50 : 4.5 nM ), and has anti-hiv activity.

AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) is a CXCR4 receptor antagonist with potential anticancer and anti-HIV activity.

Vestitol has antioxidation, anti-inflammatory and antimicrobial activities, it can strongly act in a low dose and concentration and have a promising potential to be applied in the pharmaceutical and food industries. Vestitol inhibits neutrophils migration

Eldelumab (BMS-936557) is a humanized anti-IP-10 IgG type 1 monoclonal antibody with inhibitory activity against CXCL10.Eldelumab has anti-inflammatory activity and selectively binds to CXCL10 and can be used in the study of rheumatoid arthritis, ulcerative colitis, and Crohn's disease.

Pentixafor is a peptide that selectively targets the CXCR4 receptor and can be labeled with Gallium-68 (68Ga) for visualization using positron emission tomography (PET) imaging [1].

SRT3190 is an antagonist of CXCR2.

CXCR7 antagonist-1 is a specific antagonist of the binding of the SDF-1 chemokine or I-TAC to the chemokine receptor CXCR7. CXCR7 antagonist-1 prevents tumor cell proliferation and tumor formation and can be used in studies about inflammatory diseases.

Balixafortide TFA (POL6326 TFA) is a selective, well-tolerated peptidic CXCR4 antagonist (IC50 < 10 nM). It shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium fl

Tannic acid (Gallotannic acid) is a novel hERG channel blocker.

MSX-130 is CXCR4 Antagonist.

Mavorixafor (AMD-070) is an effective and selective antagonist of CXCR4, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. Mavorixafor inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells (IC50 = 1 nM) and PBMCs (IC50 = 9 nM).

Delmetacin (Demethacin) is a non-steroidal anti-inflammatory compound with anti-inflammatory and analgesic activity and inhibitory effects on the CXC chemokine receptor CXCR1.

E70K, a CXCL8 C-terminal peptide, features a lysine (K) substitution for glutamic acid (E) at position 70 and has demonstrated the ability to attenuate neutrophil adhesion and migration in the context of inflammation [1].

SCH 563705 is an effective and orally available CXCR2 and CXCR1 antagonist (IC50s: 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively).

ITIC-4F, an indacenodithienothiophene (IDTT)-based postfullerene electron acceptor, exhibits wide applicability in high-efficiency binary and ternary single-junction as well as tandem polymer solar cells (PSCs).

Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM and it is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2]. Balixafortide blocks β-arresti

AZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2, and potentially protects against SARS-CoV-2-induced neuronal damage, preventing worsening of nociceptive sensitization and microglial activation in a migraine model of rats following seizures.

IT1t dihydrochloride inhibits CXCL12/CXCR4 interaction with IC50 of 2.1 nM. IT1t dihydrochloride is an antagonist of CXCR4.

JMS-17-2 is a potent and selective antagonist of CX3CR1( IC50 : 0.32 nM).

VUF11207 fumarate is an agonist of CXCR7 and a high-potency ligand of CXCR7 (pKi: 8.1).

CXCR4-IN-1 (Example C5), with an IC50 of 20 nM, is a potent inhibitor of CXCR4, applicable for the research of various conditions such as cancer, HIV, diabetic retinopathy, and inflammation [1].

DOTA-CXCR4-L, a peptide targeting the CXCR4 receptor, is utilized in cancer research, notably in the contexts of glioblastoma and triple-negative breast cancer [1].

VUF-11222 is a CXCR3 nonmimetic peptide agonist that induces gliosis.VUF 11222 has been used in the study of retinal inflammation.

NUCC-390 dihydrochloride is selective agonist of small-molecule CXCR4 receptor.

Ulocuplumab (BMS-936564) is a fully human anti-CXCR4 IgG4 antibody.Ulocplumab exhibits antitumor activity in acute myeloid leukemia (AML), non-Hodgkin's lymphoma (NHL), and multiple myeloma transplantation models.Ulocplumab inhibits the migration of chronic lymphocytic leukemia (CLL) cells under CXCR4 activation, induces apoptosis, and inhibits the growth and migration of cancer cells. Ulocplumab inhibits CXCL12-mediated chronic lymphocytic leukemia (CLL) cell migration in response to CXCR4 activation and induces apoptosis.)

Plerixafor octahydrochloride (JM3100 octahydrochloride) blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation. Plerixafor is a bicyclam with hematopoietic stem cell-mobilizing activity.

Motixafortide (BKT140 4-fluorobenzoyl) is an antagonist of CXCR4 (IC50: 1 nM).

TAK-779 (Takeda 779) is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).

ML339 a selective inhibitor of CXCR6(IC50 = 140 nM) with no response when screened against CXCR5 and CXCR4.

MSX-127 elicites positive response in peptide CXCR4.

SRT3109 is a CXCR2 ligand used in the treatment of chemokine mediated diseases and conditions.

CXCR4-IN-2 (compound A1), a potent bifunctional fluorinated small molecule, inhibits CXCR4 and exhibits anticancer properties by exerting cytotoxicity (IC 50: 60 μg/mL; 72 h) and antiproliferative effects on mouse colorectal cancer (CRC) cells. It induces G2/M phase cell cycle arrest and apoptosis [1].