CXCR

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

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

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

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.

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

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

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.

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

<p>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.</p>

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

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

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

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

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

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.

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

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

<p>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.</p>

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.

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.

<p>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).</p>

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.

<p>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.</p>

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

CX4338 is a CXCL8-mediated chemotaxis inhibitor.

<p>A unique collection of xnum chemokines or chemokine receptors targeted compounds for high throughput and high content screening;</p>

<p>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</p>

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.

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

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).

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

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

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

<p>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.</p>

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.

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

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

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.

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

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

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

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.

<p>CXCR4 antagonist 2 is a CXCR4 antagonist with an IC 50 value of 47 nM.</p>

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

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

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

ATI-2341, pepducin targeting the CXCR4, is an allosteric agonist activating the Gi to promote inhibition of cAMP production and induce calcium mobilization.

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

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

CXCR2 antagonist 8 is a selective CXCR2 antagonist, which can be used for the treatment and prevention of insulin resistance.

<p>Peptide R (TFA) is a synthetic and specific CXCR4 antagonist. It demonstrates excellent tumor stroma remodeling capabilities and is applicable in research on solid tumors, such as glioblastoma.</p>

<p>ACT-1004-1239 is a CXCR7 antagonist with immunomodulatory and myelination-promoting effects, used for research on inflammatory demyelinating diseases.</p>

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

NUCC-390, a selective CXCR4 agonist, promotes nerve repair by inducing CXCR4 internalization, opposite to AMD3100.

JMS-17-2 hydrochloride: potent CX3CR1 blocker, IC50 of 0.32 nM, hinders breast cancer metastasis.

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

Decursin: potential antiepileptic, hepatoprotective, anti-cancer, anti-amnesic; affects NOX activation, PKCα/MAPK/NF-κB pathways, AChE.

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

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

Reparixin inhibits CXCR1 (IC50=1 nM) strongly, CXCR2 weakly (IC50=100 nM), and it's a CXCL8 receptor blocker.

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

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

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

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

SX-682 is an orally available allosteric inhibitor of CXCR1 and CXCR2.Cost-effective and quality-assured.

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

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

Mavorixafor trihydrochloride blocks CXCR4 (IC50: 13 nM) and suppresses T-tropic HIV-1 replication (IC50: 1-9 nM). It's orally active.

Nicotinamide N-oxide, a metabolite of nicotinamide and precursor to NAD+, is reduced by liver enzyme xanthine oxidase.

Elubrixin is a interleukin 8 inhibitor and CXCR2 selective antagonist.

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

Plerixafor octahydrochloride mobilizes HSCs by blocking SDF-1alpha/CXCR4 interaction, facilitating their release into circulation.

MSX-127 elicites positive response in peptide CXCR4.

ATI-2341 acetate is an effective allosteric agonist of CXCR4, it activates Gα1 instead of Gα13.

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

USL311 blocks CXCR4/SDF-1 interaction, inhibits tumor cell growth and migration.

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

<p>SB-265610 (GSK-CXCR2) is a nonpeptide and allosteric CXCR2 antagonist.</p>

Navarixin (MK-7123)(SCH527123) is a novel, selective CXC chemokine receptor 2(CXCR2) antagonist that inhibits neutrophil activation and modulates neutrophil

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

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

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

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

MSX-130 is CXCR4 Antagonist.

ML 145 is a selective antagonist of GPR35/CXCR8 (IC50/EC50 of 20.1 nM)

CXCR4 modulator-2 (Z7R) has high potency (IC50: 1.25 nM), stable in mouse serum (t1/2=77.1 min), and anti-inflammatory in mice.

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

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

PS372424 is a specific agonist of human CXCR3, with anti-inflammatory activity.

<p>AZ10397767: Potent CXCR2 blocker (IC50=1nM); lowers neutrophil infiltration in tumors in vitro/in vivo.</p>

AMD 3465 (GENZ-644494) blocks CXCR4, hinders X4 HIV replication (IC50: 1-10 nM), ineffective against R5 viruses, IC50: 0.75 nM (12G5 mAb), 18 nM (CXCL12AF647).

GPR35 agonist 1 is a highly effective and specific GPR35/CXCR8 agonist (EC50: 5.8 nM).

CXCR4 antagonist

SB02024 inhibits VPS34, boosts cGAS-STING, hinders autophagy, and shrinks breast cancer xenografts; enhances Sunitinib/Erlotinib efficacy.

ACT-660602: Oral CXCR3 blocker, T-cell migration inhibitor, effective in acute lung injury models, potential for autoimmune research. IC50: 204 nM.

CXCR4 antagonist with IC50 of 8.8 nM, inhibits CXCL12-induced calcium increase and chemotaxis, with good safety and minimal CYP, hERG impact.

CXCR3 antagonist 6c blocks CXCR3 and inhibits Ca2+ movement and T-cell migration (IC50: 0.06 µM & 100 nM) with selectivity over 14 other GPCRs.

CXCR4 antagonist 9, with IC50s of 15 nM & 1.3 nM against CXCR4 & Ca²⁺ rise by CXCL12 respectively.

<p>VUF10132 is a full inverse CXCR3 N3.35A agonist.</p>

AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an CXCR3 antagonist.