CXCR

CXC chemokine receptors (CXCRs) are seven-transmembrane chemokine receptors that regulate immune-system development and leukocyte trafficking through chemokine-directed cell migration^[1]. Mechanistically, CXCR signaling connects ligand recognition to immune-cell positioning, with CXCL8-CXCR1/CXCR2 driving neutrophil chemotaxis during infection and tissue injury^[2]. In disease and experimental models, CXCR4 binds CXCL12/SDF-1, supports chemotaxis and calcium signaling, and functions as the HIV-1 entry cofactor LESTR/fusin^[3]. Compared with related isoforms, CXCR3-A and CXCR3-B show divergent activities: CXCR3-B mediates endothelial growth inhibition induced by CXCL9, CXCL10, CXCL11, and CXCL4^[4]. CXCR5 differs functionally by mediating selective B-lymphocyte attraction through BCA-1/CXCL13, linking this receptor to lymphoid-tissue B-cell trafficking^[5]. For experimental applications, plerixafor/AMD3100 provides a validated CXCR4 antagonist tool that rapidly mobilizes CD34⁺ hematopoietic cells in healthy volunteers^[6].

References:

[1]. Bachelerie F, et al. International Union of Basic and Clinical Pharmacology. [corrected]. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors. Pharmacol Rev. 2013 Nov 11;66(1):1-79.

[2]. Cambier S, et al. The chemokines CXCL8 and CXCL12: molecular and functional properties, role in disease and efforts towards pharmacological intervention. Cell Mol Immunol. 2023 Mar;20(3):217-251.

[3]. Bleul CC, et al. The lymphocyte chemoattractant SDF-1 is a ligand for LESTR/fusin and blocks HIV-1 entry. Nature. 1996 Aug 29;382(6594):829-33. [Content Brief]

[4]. Lasagni L, et al. An alternatively spliced variant of CXCR3 mediates the inhibition of endothelial cell growth induced by IP-10, Mig, and I-TAC, and acts as functional receptor for platelet factor 4. J Exp Med. 2003;197(11):1537-49. [Content Brief]

[5]. Legler DF, et al. B cell-attracting chemokine 1, a human CXC chemokine expressed in lymphoid tissues, selectively attracts B lymphocytes via BLR1/CXCR5. J Exp Med. 1998 Feb 16;187(4):655-60. [Content Brief]

[6]. Devine SM, et al. Rapid mobilization of CD34+ cells following administration of the CXCR4 antagonist AMD3100 to patients with multiple myeloma and non-Hodgkin's lymphoma. J Clin Oncol. 2004;22(6):1095-102. [Content Brief]

CXCR Related Products (164):

By Type:	Pan (1)
By Effects:	Inhibitors (68) Agonists (8) Antagonists (35) Activator (1) Modulators (7) Inducer (1) Controls (2) Ligand (1)

Cat. No.	Product Name	Effect	Purity

HY-153549

Pentixafor		99.79%
Pentixafor is a peptide that targets CXCR4. Pentixafor is capable of being labelled with ⁶⁸Gallium (⁶⁸Ga) for positron emission tomography (PET) imaging. Pentixafor can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

HY-18981

Decursin		99.92%
Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities.

HY-100806R

Kynurenic acid (Standard)
Kynurenic acid (Standard) is the analytical standard of Kynurenic acid. This product is intended for research and analytical applications. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.

HY-19519

Ladarixin	Antagonist	99.44%
Ladarixin (DF 2156A free base) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin can be used for the research of COPD and asthma.

HY-107536

ML 145
ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC₅₀/EC₅₀ of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC₅₀/EC₅₀=21.7 μM). ML 145 has no significant activity for GPR35 at either rodent ortholog.

HY-16509

UNBS5162	Antagonist	99.07%
UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.

HY-P991761

Anti-Mouse CXCL10 Antibody (1F11)	Inhibitor
Anti-Mouse CXCL10 Antibody (1F11) reacts with the pro-inflammatory CXCL10. Anti-Mouse CXCL10 Antibody (1F11) can be used for neutralization of CXCL10 (in vitro and in vivo) and for inhibition of T cell recruitment in vivo in a range of inflammatory disease models. Recommend Isotype Controls: Polyclonal Armenian hamster IgG, Isotype Control (HY-P990305).

HY-185565

PD-1/PD-L1-IN-63	Modulator
PD-1/PD-L1-IN-63 is an orally active PD-1/PD-L1 inhibitor with an IC₅₀ of 9.1 nM. PD-1/PD-L1-IN-63 blocks the PD-1/PD-L1 interaction, induces cancer cell death and inhibits tumor growth. PD-1/PD-L1-IN-63 can be used in the research of melanoma.

HY-P99459

Baminercept	Inhibitor	99.97%
Baminercept (BG 9924; TT-47) is an Ig fusion protein targeting the lymphotoxin β receptor (LTβR). Baminercept effectively regulates subsets of circulating immune cells by inhibiting LIGHT, LT-α1β2 and their receptors. Baminercept also increases blood lymphocyte counts and reduces plasma CXCL13 levels. Baminercept carries a high risk of hepatotoxicity. Baminercept can be used in research on rheumatoid arthritis and primary Sjögren's syndrome.

HY-P99190

Eldelumab	Inhibitor	99.50%
Eldelumab (BMS-936557) is a human anti-CXCL10 (IP-10) monoclonal antibody (IgG1 type). Eldelumab selectively binds to CXCL10 and blocks CXCL10-induced calcium flux and cell migration. Eldelumab can be used in studies of autoimmune and auto-inflammatory diseases such as rheumatoid arthritis, ulcerative colitis and crohn's disease.

HY-108691

PF-06465469		99.48%
PF-06465469 is a covalent inhibitor of ITK with an IC₅₀ of 2 nM. PF-06465469 also inhibits BTK. PF-06465469 inhibits cell migration in response to CXCL12. PF-06465469 decreases PD-1 and LAG-3 expression. PF-06465469 can be used to study leukemia and T-cell lymphoma.

HY-P4911A

SDF-1α (human) TFA	Modulator	98.89%
SDF-1α (human) TFA is a mononuclear cells chemoattractant that can bind to CXCR4. SDF-1α plays a central role in stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis and ventricular remodelling following myocardial infarction. SDF-1α (human) TFA can be used in cardiovascular disease research.

HY-P990255

Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5)	Inhibitor
Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) is an anti-mouse CXCL9/MIG IgG monoclonal antibody. Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) can reduce tumor infiltration of CD8⁺ cytotoxic T cells (CTLs). Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) can prolong the survival of transplanted hearts. Anti-Mouse CXCL9/MIG Antibody (MIG-2F5.5) can be used for researches on immunology and cancer such as prostate cancer.

HY-P0172A

ATI-2341 TFA	Agonist	98.08%
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).

HY-P10300

CXCL8 (54-72)		99.90%
CXCL8 (54-72) is a C-terminal peptide based on the chemokine CXCL8. CXCL8 (54-72) has an interaction between a long and highly positively charged C-terminal region and a negative charge on the GAG that binds to the GAG. CXCL8 (54-72) can inhibit the adhesion and migration of neutrophils and adhesion of endothelial cells. CXCL8 (54-72) can be used to study chemokines in inflammatory response.

HY-15251A

(Rac)-Reparixin	Control	99.75%
(Rac)-Reparixin is the isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC₅₀s of 1 and 100 nM, respectively.

HY-P99404

Quetmolimab	Inhibitor	99.9%
Quetmolimab (E6011) is a humanized anti-Fractalkine (CX3CL1) monoclonal antibody. Quetmolimab binds to membrane-bound and soluble Fractalkine, neutralizes Fractalkine-induced migration of CX3CR1-expressing cells, mediates target-bound complex elimination from serum. Quetmolimab suppresses free soluble Fractalkine levels in cynomolgus monkeys, with target engagement linked to increased serum total Fractalkine concentration. Quetmolimab can be used for the research of Crohn’s disease, rheumatoid arthritis, and primary biliary cholangitis.

HY-175739

TFAM activator 1	Inhibitor	99.25%
TFAM activator 1 is a TFAM activator. TFAM activator 1 increases TFAM protein levels, promotes mitochondrial DNA stability, increases mitochondrial DNA copy number, and prevents mitochondrial DNA from escaping into the cytoplasm. TFAM activator 1 improves cellular energy metabolism in cybrid cells. TFAM activator 1 reduces fibrosis markers in fibroblasts. TFAM activator 1 can be used in the research of mitochondrial encephalomyopathy, lactic acidosis, and stroke-like episodes syndrome, systemic sclerosis, and autoimmune diseases.

HY-P991567

VX5	Modulator
VX5 (VX5/5261) is a humanized IgG1κ monoclonal antibody inhibitor targeting BCA-1/CXCL13. VX5 significantly inhibits human CXCL13-mediated internalization of CXCR5, blocks both human and mouse CXCL13-dependent B-cells chemotaxis and migration. VX5 can be used to study autoimmune diseases like multiple sclerosis and arthritis, and cancers like gastric lymphomas and colon cancer.

HY-160041A

Olaptesed pegol sodium	Inhibitor
Olaptesed pegol (NOX-A12) sodium is a L-oligoribonucleotide aptamer targeting CXCL12 based on a pegylated structure. Olaptesed pegol sodium neutralizes CXCL12, and CXCL12 inhibition mobilizes chronic lymphocytic leukemia cells into the circulation and prevents their homing into the protective microenvironment. Olaptesed pegol sodium can enhances the infiltration of human primary T cells and NK cells and inhibit tumor growth companied with anti-PD-1 antibody. Olaptesed pegol sodium can be used for researches of colon cancer and lymphocytic leukemia.

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