CXCR4
CXCR4 is a G protein-coupled chemokine receptor that mediates migration of resting leukocytes and hematopoietic progenitors in response to SDF-1/CXCL12[1]. Mechanistically, CXCR4-CXCL12 signaling supports hematopoiesis and cerebellar development, and CXCR4-deficient mice show hematopoietic and cardiac defects matching SDF-1-deficient mice[1]. In vascular development, mice lacking CXCR4 or PBSF/SDF-1 show defective formation of large vessels supplying the gastrointestinal tract, identifying this axis as a signaling system for organ vascularization[2]. In disease models, CXCR4 and CCR7 are highly expressed in human breast cancer cells, malignant breast tumors, and metastases, linking chemokine receptor programs to tumor cell migration and metastatic spread[3]. Compared with the related ACKR3/CXCR7 receptor, CXCR4 couples to G proteins and directly promotes cell migration, whereas ACKR3 is G protein-independent and scavenges CXCL12 to regulate extracellular chemokine levels[4]. For experimental applications, CXCR4 antagonist structures with IT1t and CVX15 define ligand-binding sites near the extracellular surface, supporting structure-guided inhibitor design[5]. AMD3100 selectively antagonizes CXCR4 and rapidly mobilizes murine and human hematopoietic progenitor cells, especially with G-CSF[6].
References:
- [1]. Zou YR, et al. Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development. Nature. 1998 Jun 11;393(6685):595-9. [Content Brief]
- [2]. Tachibana K, et al. The chemokine receptor CXCR4 is essential for vascularization of the gastrointestinal tract. Nature. 1998 Jun 11;393(6685):591-4. [Content Brief]
- [3]. Müller A, et al. Involvement of chemokine receptors in breast cancer metastasis. Nature. 2001 Mar 1;410(6824):50-6. [Content Brief]
- [4]. Schafer CT, et al. Distinct Activation Mechanisms of CXCR4 and ACKR3 Revealed by Single-Molecule Analysis of their Conformational Landscapes. bioRxiv [Preprint]. 2025 Feb 6:2023.10.31.564925. [Content Brief]
- [5]. Wu B, et al. Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science. 2010 Nov 19;330(6007):1066-71. [Content Brief]
- [6]. Broxmeyer HE, et al. Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist. J Exp Med. 2005 Apr 18;201(8):1307-18. [Content Brief]
-
CXCR4 Related Products (82)
Related Products (82)
-
Recombinant Proteins (6)
-
Antibodies (1)
-
CXCR4 antagonist 10
0 ImagesCXCR4 antagonist 10 (compound 21) is a potent antagonist of CXCR4, with the IC50 of 7.8 nM. CXCR4 antagonist 10 plays an important role in cancer research.
-
Peptide R
0 ImagesCat. No.: HY-P4111CAS No.: 1318232-11-9Peptide R is a cyclic peptide and a specific CXCR4 antagonist. Peptide R exhibits excellent ability to effectively remodel tumor stroma. Peptide R has potential for use in tumor research.
-
Peptide R TFA
0 ImagesCat. No.: HY-P4111APurity: 98.34%Peptide R (TFA) is a synthetic and specific CXCR4 antagonist. Peptide R (TFA) shows outstanding capacities to remodel the tumor stroma. Peptide R (TFA) can be used for solid tumor (glioblastoma, etc.) research.
-
Hit 14
0 ImagesCat. No.: HY-162632CAS No.: 440338-68-1Hit 14 is an inhibitor for C-X-C chemokine receptor type 4 (CXCR4) with IC50 of 254 nM. Hit 14 inhibits the migration and invasion of cell MDA-MB-231. Hit 14 inhibits the Akt phosphorylation, exhibits anti-inflammatory activity, and ameliorateds the ear swelling and damage in mouse models.
-
Peptide R analogue 10
0 ImagesPeptide R analogue 10 (compound 10) is an analog of the CXCR4 antagonist peptide Peptide R (HY-P4111) with stronger antagonistic potency, specificity and plasma stability. Peptide R analogue 10 can inhibit CXCL12-mediated cell migration, ERK phosphorylation and CXCR4 internalization. Peptide R analogue 10 can be used in the study of CXCR4 overexpressing leukemia and colon cancer.
-
ALX 40-4C
0 ImagesCat. No.: HY-P7061CAS No.: 143413-49-4
-
CXCR4 antagonist 9
0 ImagesCat. No.: HY-147979CAS No.: 2304750-83-0CXCR4 antagonist 9 (Compound 2) is a CXCR4 antagonist with an IC50 of 15 nM. CXCR4 antagonist 9 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 1.3 nM.
-
Nef-M1
0 ImagesNef-M1 (Nef-Motif-1) is an antagonist peptide targeting CXCR4 and an apoptosis inducer derived from a myristoylated protein encoded by the nef gene in HIV. Nef-M1 inhibits tumor angiogenesis and epithelial-mesenchymal transition (EMT). Nef-M1 activates the apoptosis pathway by increasing the level of caspase-3 in cancer cells. Nef-M1 simultaneously inhibits VEGF-A, p-GSK-3β and vimentin, and enhances E-cadherin, thereby inhibiting angiogenesis and EMT processes. Nef-M1 can be used in the study of colorectal cancer and breast cancer.
-
FC131
0 ImagesFC131 is a CXCR4 antagonist that inhibits AKT kinase activity in AML OCI-AML3 cells. D-ArgFC131, a derivative of FC131, inhibits the phosphorylation of downstream ERK1/2 and Akt, induces caspase-3 pathway-mediated apoptosis, and causes cell cycle arrest. FC131 exerts cytotoxic effects in cancer cells such as AML cells. FC131 is applicable for cancer-related research.
-
LY-2624587
0 ImagesCat. No.: HY-P991656CAS No.: 2125546-89-4LY-2624587 is a humanized IgG4 monoclonal antibody antagonist targeting CXCR4. LY-2624587 blocks SDF-1/CXCR4 interaction and SDF-1-induced GTP binding. LY-2624587 significantly inhibits cell migration and induces apoptosis in human lymphoma and leukemia cells. LY-2624587 also inhibits CXCR4 and SDF-1 mediated cell signaling including activation of MAPK and AKT. LY-2624587 can be used for human hematological malignancies like acute myeloid leukemia (AML) research.
-
CXCR4 antagonist 7
0 ImagesCat. No.: HY-147808CAS No.: 1185451-72-2CXCR4 antagonist 7 (Compound PARA-B) is a CXCR4 antagonist with the IC50 of 9.3 nM. CXCR4 antagonist 7 can be used for the research of HIV infection, inflammatory diseases, cancer, and WHIM syndrome.
-
BPRCX807
0 ImagesCat. No.: HY-178205CAS No.: 2236595-58-5BPRCX 807 is a selective and potent CXCR4 (CXC chemokine receptor type 4) antagonist. BPRCX 807 inhibits CXCL12-mediated ERK and Akt phosphorylation. BPRCX 807 can significantly suppress primary tumor growth. BPRCX 807 can be used for the study of hepatocellular carcinoma.
-
CTCE-9908 TFA
0 ImagesCat. No.: HY-P1103ACTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.
-
CXCR4 modulator-1
0 ImagesCat. No.: HY-146053CAS No.: 2987682-11-9CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator with an EC50 value of 100 nM. CXCR4 modulator-1 can be used for researching anti-inflammatory, anticancer and anti-HIV.
-
CXCR4 antagonist 3
0 ImagesCat. No.: HY-144286CAS No.: 2761009-43-0CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus.
-
Cyclazosin
0 ImagesCat. No.: HY-184086CAS No.: 139953-73-4Cyclazosin is an α1D-adrenergic receptor antagonist and a partial agonist of CXCR4/ACKR3. The pKi values of Cyclazosin for cloned human α1D, α1B and α1A adrenergic receptors are 9.28, 9.23 and 8.18, respectively. Cyclazosin induces β-arrestin recruitment in CXCR4 and ACKR3 with EC50 values of 16 μM and 10 μM, respectively, stimulates ERK1/2 phosphorylation, and induces receptor internalization. Cyclazosin potently inhibits CXCL12-induced chemotaxis of primary human aortic vascular smooth muscle cells. Cyclazosin alters MDMA-induced thermoregulatory responses in mice, converting monophasic hyperthermia to a biphasic pattern without affecting resting core body temperature. Cyclazosin can be used for diseases related to tumor metastasis, MDMA-induced hyperthermia and vasoconstriction.
-
UCUF-965
0 ImagesCat. No.: HY-182850CAS No.: 2965316-77-0UCUF-965 is a CXCR4 positive allosteric modulator. UCUF-965 potentiates CXCL12-induced β-arrestin recruitment and cAMP signaling, activates lymphoblast migration, induces calcium flux, and does not bind CXCR4’s orthosteric CXCL12 site. UCUF-965 reduces miR-15b and miR-29a levels, increases miR-146a levels in fibroblasts. UCUF-965 enhances angiogenesis and reduces wound healing time in diabetic mice. UCUF-965 can be used for the research of diabetic wound healing impairment.
