CXCR

SX-682 is an orally available allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor myeloid suppressor cell recruitment and enhances T cell activation and anti-tumor immunity, with the potential to treat castration-resistant prostate cancer.

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

AZD-5069 is an chemokine receptor 2 antagonist (CXCR2; IC50 = 0.79 nM).

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

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).

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

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.

Navarixin (MK-7123)(SCH527123) is a novel, selective CXC chemokine receptor 2(CXCR2) antagonist that inhibits neutrophil activation and modulates neutrophil trafficking in animal models, characteristics that may be beneficial in the treatment of conditions with unbalanced pulmonary neutrophilia.

AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.

SB-265610 (GSK-CXCR2) is a nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis (IC50s: 3.7 nM and 70 nM, respectively).

UNBS5162 (UNBS-5162) is a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers.

Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.

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.

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.

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

Reparixin (Repertaxin) is a potent inhibitor of both CXCL8 receptors CXCR1 2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).

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.

USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4. USL311 inhibits CXCR4 activation and decreases proliferation and migration of CXCR4-expressing tumor cells, with anti-tumor activ

Danirixin (GSK1325756) is a potent antagonist of CXCR2 that inhibits IL-8 binding to CXCR2 (IC50: 12.5 nM).

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

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

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

SCH 546738 is an orally available, selective and potent CXCR3 antagonist that attenuates the development of autoimmune diseases and delays graft rejection.

MSX-122 is a novel small molecule and partial CXCR4 antagonist, with potent inhibition of CXCR4/CXCL12 actions(IC50 = 10 nM).

Baohuoside I (Icariside-II) is a component of Epimedium koreanum, exhibits anti-inflammatory activity and anti-osteoporosis activities.

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.

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.

MSX-130 is CXCR4 Antagonist.

LIT927 (LIT-927) is an orally active CXCL12 neutraligand (Ki: 267 nM for CXCL12 binding to CXCR4).

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.

Ac-Pro-Gly-Pro-OH is an acetyl-modified tripeptide compound that acts as a CXCR2 agonist, exhibiting bactericidal and anti-inflammatory activities. It inhibits apoptosis of immune cells, suppresses the production of pro-inflammatory cytokines, and has been utilized in studies of sepsis and lung inflammation.

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

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

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

Nicotinamide N-oxide (Nicotinamide 1-oxide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. The enzyme that catalyzes the reduction of nicotinamide N-oxide to nicotinamide in the liver is xanthine oxidase.

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

MSX-127 elicites positive response in peptide CXCR4.

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

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).

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.

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

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

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.

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.

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

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

WZ811 is a novel and effective small molecular CXCR4 antagonist (EC50: 0.3 nM).

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.