CXCR

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

CXCR7 modulator 1 is an effective and orally bioavailable peptoid hybrid CXCR7 modulator with Ki of 9 nM.

CXCR7 modulator 2 is a 7-type C-X-C chemokine receptor (CXCR7) modulator with a Ki of 13 nM.

(R,R)-CXCR2-IN-2, a diastereoisomer of CXCR2-IN-2 (compound 68), is a brain-penetrant CXCR2 antagonist with a pIC50 of 9 in the Tango assay and 6.8 in the HWB Gro-α induced CD11b expression assay[1].

CXCR2-IN-2 (compound 68) is a highly selective CXCR2 antagonist (IC50=5.2 nM) with the advantages of blood-brain barrier penetration and oral bioavailability. It inhibits Gro-α-induced CD11b expression in human whole blood (IC50=0.04 μM).

CXCR3 antagonist 6c is an antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3).1It inhibits calcium mobilization induced by chemokine (C-X-C motif) ligand 11 (CXCL11) in HEK293 cells expressing the human receptor (IC50= 0.06 μM). It is selective for CXCR3 over a panel of 14 human G protein-coupled receptors at 10 μM. CXCR3 antagonist 6c inhibits CXCR3-mediated migration of isolated human T cells (IC50= ~100 nM). 1.Cole, A.G., Stroke, I.L., Brescia, M.-R., et al.Identification and initial evaluation of 4-N-aryl-[1,4]diazepane ureas as potent CXCR3 antagonistsBioorg. Med. Chem. Lett.16(1)200-203(2006)

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.

CXCR4 antagonist 1 is a potent inhibitor of the CXCR4 receptor with notable anti-HIV activity.

CXCL-CXCR1/2-IN-1 is an orally active and potent inhibitor of the ELR+CXCL-CXCR1/2 pathway with anticancer and anti-angiogenic activity and can be used to study cardiovascular disease and cancer.

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.

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.

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

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.

MSX-127 elicites positive response in peptide CXCR4.

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.

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

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

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).

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

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

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

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

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