CXCR

AMG 487: potent CXCR3 antagonist, blocks CXCL10/CXCL11 binding, IC50s: 8.0/8.2 nM.

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

Delmetacin: a non-steroidal anti-inflammatory drug with analgesic properties, inhibits CXCR1.

Eldelumab (BMS-936557) is an anti-IP-10 IgG 1 monoclonal antibody.Eldelumab has anti-inflammatory activity and is used to study rheumatoid arthritis.

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.

Quetmolimab is a humanized monoclonal antibody targeting chemokine ligand 1 (CX3CL1) that can be used to study rheumatoid arthritis.

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

Motixafortide TFA is a CXCR4 antagonist with ~1 nM IC50, promoting AML apoptosis by modulating miR-15a/16-1 and downregulating ERK and BCL-2.

VUF-11222 is an agonist of high affinity non-peptide CXCR3 agonist (pKi = 7.2).

CXCL8 (54-72) is a C-terminal peptide segment of the chemokine CXCL8. This peptide features a long, highly positively charged C-terminal region that interacts with the negative charges on glycosaminoglycans (GAG) to facilitate binding. CXCL8 (54-72) inhibits neutrophil adhesion and migration, as well as adhesion to endothelial cells. It is useful in studying the role of chemokines in inflammatory responses.

HuMax-IL8 (MDX 018) is a humanized anti-IL-8 monoclonal antibody for the study of metastatic or unresectable solid tumors.

CXCR4-IN-3 (compound XVI) is an orally active inhibitor targeting the inflammation-related receptor CXCR4, with an IC50 of 3.2 nM. It exhibits potent anti-chemotactic effects, with an inhibition rate of 79.19±2.33%. Additionally, CXCR4-IN-3 possesses anti-inflammatory properties and can be utilized in research on IBD (inflammatory bowel disease).

MKEY peptide inhibits CXCL4-CCL5, reduces atherosclerosis and aneurysm, neuroinflammatory effects unknown.

CX4338 is a CXCL8-mediated chemotaxis inhibitor.

CXCR4 blocker; triggers cell division failure in ovarian cancer, boosts taxol and docetaxel treatment effects, proven in mice.

Balixafortide TFA is a selective CXCR4 antagonist with IC50 < 10nM, over 1000x preference for CXCR4, and blocks β-arrestin and calcium flux.

ITIC-4F: a postfullerene IDTT electron acceptor for high-efficiency PSCs, relevant in binary, ternary, and tandem setups.

Vimnerixin (AZD4721) is an orally administered CXCR2 antagonist for inflammation studies.

SDF-1α (human) serves as a chemotactic agent for mononuclear cells through its interaction with the CXCR4 receptor, facilitating critical biological processes

ACKR3 agonist 1 (compound 27), exhibiting selective agonistic properties for ACKR3 (EC 50 =69 nM, E max =82%), demonstrates the capability to inhibit platelet aggregation and shows potential in mitigating platelet-mediated thrombosis. This compound is characterized by its metabolic stability and non-cytotoxic nature.

CXCL-CXCR1/2-IN-1 is an ELR+CXCL-CXCR1/2 pathway inhibitor with anticancer activity and can be used in the study of cardiovascular disease.

CXCR4 antagonist and ACKR3 (CXCR7) agonist (EC50 = 350 nM for CXCR7).

CCR7 antagonist1 (30c) functions as a dual antagonist, targeting CXCR2 with an IC50 of 11.02 μM and CCR7 with an IC50 of 0.43 μM.

CXCR2Probe 1 (Compound[18F]16b) is a selective ligand for CXCR2 and serves as a radioactive tracer for PET imaging of neutrophils in inflammatory diseases.

PDE4-IN-1 is a PDE4 inhibitor characterized by high potency (IC50: 8.6 nM) and superior selectivity over other PDE subtypes. This compound inhibits the release of inflammatory cytokines and chemokines. Additionally, PDE4-IN-1 significantly restores the damaged cAMP-CREB signaling pathway, inhibits proliferation, and promotes differentiation to reverse psoriasis formation.

CXCR4 antagonist 2 is a CXCR4 antagonist with an IC 50 value of 47 nM.

NI-0801 (Anti-CXCL10 / IP-1) is a CHO-expressed humanized monoclonal antibody targeting CXCL10/IP-10 for the study of vitiligo and biliary cirrhosis.

RCP168 is a highly selective and potent CXCR4 receptor antagonist with an IC50 of 5 nM. It exhibits superior capacity to inhibit HIV-1 (Human Immunodeficiency Virus type 1) from entering host cells via the CXCR4 receptor compared to natural chemokines. RCP168 suppresses HIV-1 infection by blocking viral binding sites or inducing receptor internalization. It can be utilized in research to study interactions between the CXCR4 receptor and other chemokine receptors.

PF-06835375 is a humanized IgG1 antibody that selectively targets CXCR5 expressed on B cells, Tfh cells, and circulating Tfh-like cells (cTfh). It is applicable for research into systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA).

BVT173187 is a neutrophil formyl peptide receptors (FPR1) inhibitor.

TC14012 TFA is a peptide-mimetic CXCR4 antagonist and CXCR7 agonist that promotes the recruitment of β-arrestin by CXCR7 .

4-Amino-D-phenylalanine ([D-Phe(4-NH2)]) is a cyclic pentapeptide that inhibits the binding of CXCL12 to CXCR4 in FC131, with an IC50 value of 0.1 μM.

VB-85247 is a STING agonist that, by activating the STING pathway, induces the upregulation of inflammatory cytokines IFNα/β, TNFα, IL6, and CXCL10, as well as the maturation and activation of dendritic cells. It can lead to the regression of tumors within the bladder and is applicable in bladder cancer research.

Peptide R54 (Pep R54; CXCR4 antagonist peptide 19) is an antagonistic polypeptide targeting CXCR4, known for its significant anticancer properties. It inhibits CXCR4-dependent cell migration, epithelial-mesenchymal transition, and the development of lung metastasis, offering better serum stability and higher CXCR4 affinity (IC50=20 nM) compared to the lead compound. Peptide R54 works synergistically with anti-PD-1 therapy to exhibit antitumor effects in vivo, enhancing granzyme activity and reducing Foxp3 cell infiltration. It is useful for research in colon cancer, ovarian cancer, and melanoma.

Peptide 78 is identical to peptide 74 except that serine replaces cysteine. It does not inhibit 72-kDa type IV collagenase.

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

CXCL12 ligand 1 is the first ligand of the sY12-binding pocket on chemokine CXCL12 .

ABX-IL8 is a humanized antibody targeting IL-8, capable of interfering with tube formation in human umbilical vein endothelial cells.

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

KRH-3955 hydrochloride is an orally available CXCR4 blocker with IC50 of 0.61 nM and EC50 of 0.3-1.0 nM against X4 HIV-1.

Peptide R, a cyclic CXCR4 antagonist, remodels tumor stroma, aiding cancer research.

T140, a Polyphemusin II-derived peptide, inhibits HIV-1 entry and blocks anti-CXCR4 antibody (12G5) binding.

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

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

vMIP-II (1-21) (NT21MP) TFA (TFA is a potent inhibitor of CXCR4. This compound interacts broadly with CC and CXC chemokine receptors. Furthermore, vMIP-II (1-21) TFA inhibits CXCR4 by competing for binding sites with 125I-SDF-1R, exhibiting an IC50 value of 190 nM.

"ITIC, a non-fullerene acceptor with high Tg of 180°C, shows excellent thermal stability and a low glass-crystal transition, plus unique crystallization."

Bam 12P is a Pro-Met-enkephalin precursor that is isolated from the bovine adrenal medulla.

PS372424 hydrochloride,CXCR3 agonist. Anti-inflammatory. Inhibits T-cell migration.

LY2510924 is an effective and selective CXCR4 antagonist. It blocks SDF-1 binding to CXCR4 (IC50: 0.079 nM).