CCR2
CCR2 is a CC chemokine receptor that mediates MCP-1/CCL2-dependent monocyte chemotaxis, receptor binding, and ligand internalization in inflammatory and vascular contexts[1][2]. Mechanistically, the CCR2 amino-terminal domain is necessary and sufficient for high-affinity MCP-1 binding, while tyrosine sulfation enhances CCR2 interaction with monomeric and dimeric MCP-1 and supports leukocyte recruitment[1][3]. In human monocytes, LDL increases CCR2 expression and strengthens MCP-1 chemotactic responses, linking CCR2 signaling to monocyte recruitment during atherogenesis[4]. In disease models, leukocyte-derived CCR2 is critical for angiotensin II-accelerated atherosclerosis and aneurysm formation in hypercholesterolemic mice[5]. CCR2 also mediates MCP-1 binding and internalization along brain microvessels, supporting its use in blood-brain barrier and neuroinflammation models[6]. Compared with related isoforms, CCR2A and CCR2B show cell-specific distribution in idiopathic inflammatory myopathies, where CCR2A appears in vessel walls and mononuclear cells, while CCR2B appears in satellite cells, neuromuscular junction domains, and regenerative fibers[7]. For experimental applications, MCP-1 binds and activates CCR2B as a monomer, and CCR2-blocking antibodies reduce myeloma-cell migration toward bone marrow stromal chemokines[8][9].
References:
- [1]. Monteclaro FS, et al. The amino-terminal domain of CCR2 is both necessary and sufficient for high affinity binding of monocyte chemoattractant protein 1. Receptor activation by a pseudo-tethered ligand. J Biol Chem. 1997 Sep 12;272(37):23186-90. [Content Brief]
- [2]. Preobrazhensky AA, et al. Monocyte chemotactic protein-1 receptor CCR2B is a glycoprotein that has tyrosine sulfation in a conserved extracellular N-terminal region. J Immunol. 2000 Nov 1;165(9):5295-303. [Content Brief]
- [3]. Tan JHY, et al. Tyrosine sulfation of chemokine receptor CCR2 enhances interactions with both monomeric and dimeric forms of the chemokine monocyte chemoattractant protein-1 (MCP-1). J Biol Chem. 2013 Apr 5;288(14):10024-10034. [Content Brief]
- [4]. Han KH, et al. Chemokine receptor CCR2 expression and monocyte chemoattractant protein-1-mediated chemotaxis in human monocytes. A regulatory role for plasma LDL. Arterioscler Thromb Vasc Biol. 1998 Dec;18(12):1983-91. [Content Brief]
- [5]. Ishibashi M, et al. Bone marrow-derived monocyte chemoattractant protein-1 receptor CCR2 is critical in angiotensin II-induced acceleration of atherosclerosis and aneurysm formation in hypercholesterolemic mice. Arterioscler Thromb Vasc Biol. 2004 Nov;24(11):e174-8. [Content Brief]
- [6]. Dzenko KA, et al. The chemokine receptor CCR2 mediates the binding and internalization of monocyte chemoattractant protein-1 along brain microvessels. J Neurosci. 2001 Dec 1;21(23):9214-23. [Content Brief]
- [7]. Bartoli C, et al. CCR2A and CCR2B, the two isoforms of the monocyte chemoattractant protein-1 receptor are up-regulated and expressed by different cell subsets in idiopathic inflammatory myopathies. Acta Neuropathol. 2001 Oct;102(4):385-92. [Content Brief]
- [8]. Paavola CD, et al. Monomeric monocyte chemoattractant protein-1 (MCP-1) binds and activates the MCP-1 receptor CCR2B. J Biol Chem. 1998 Dec 11;273(50):33157-65. [Content Brief]
- [9]. Vande Broek I, et al. Chemokine receptor CCR2 is expressed by human multiple myeloma cells and mediates migration to bone marrow stromal cell-produced monocyte chemotactic proteins MCP-1, -2 and -3. Br J Cancer. 2003 Mar 24;88(6):855-62. [Content Brief]
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CCR2 Related Products (53)
Related Products (53)
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Recombinant Proteins (3)
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Antibodies (1)
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Anti-CCL2 (Carlumab)-SMCC-DM1
0 ImagesCat. No.: HY-171680Anti-CCL2 (Carlumab)-SMCC-DM1 is an antibody-drug conjugate (ADC) consisting of the humanized anti-CCL2 (chemokine ligand 2) antibody Carlumab (HY-P99188) conjugated to the linker SMCC (HY-42360) and the cytotoxic microtubule inhibitor DM1 (HY-19792). The ADC toxic molecule and linker part are SMCC-DM1 (HY-101070). Anti-CCL2 (Carlumab)-SMCC-DM1 can be used in the research of cancer, especially prostate cancer.
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Anti-CCL2 (Carlumab)-SPDB-DM4
0 ImagesCat. No.: HY-171681Anti-CCL2 (Carlumab)-SPDB-DM4 is an antibody-drug conjugate (ADC) consisting of the humanized anti-CCL2 (chemokine ligand 2) antibody Carlumab (HY-P99188) conjugated with the linker SPDB (HY-12448) and the tubulin inhibitor DM4 (HY-12454). The ADC toxic molecule and linker part are sulfo-SPDB-DM4 (HY-101141). Anti-CCL2 (Carlumab)-SPDB-DM4 can be used in cancer research.
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Anti-CCL2 (Carlumab)-MC-Vc-PAB-SN38
0 ImagesCat. No.: HY-171684Anti-CCL2 (Carlumab)-MC-Vc-PAB-SN38 is an antibody-drug conjugate (ADC) consisting of the humanized anti-CCL2 (chemokine ligand 2) antibody Carlumab (HY-P99188) conjugated to the linker Mc-VC-PAB and the topoisomerase I inhibitor SN38 (HY-13704). The ADC toxic molecule and linker part are Mc-VC-PAB-SN38 (HY-131057). Anti-CCL2 (Carlumab)-MC-Vc-PAB-SN38 can be used in cancer research.
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RO5234444
0 ImagesCat. No.: HY-100819CAS No.: 1365266-79-0RO5234444 is an orally active CCR2 antagonist, with IC50s of 22nM for human CCR2 and 161 nM for mouse CCR2. RO5234444 alleviates glomerulosclerosis, reduces albuminuria, and significantly improves the glomerular filtration rate (GFR) in the uninephrectomized (1K) type 2 diabetic db/db mouse model. RO5234444 can be used for the study of type 2 diabetic nephropathy.
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Anti-CCL2 (Carlumab)-McMMAF
0 ImagesCat. No.: HY-171682Anti-CCL2 (Carlumab)-McMMAF is an antibody-drug conjugate (ADC) consisting of the humanized anti-CCL2 (chemokine ligand 2) antibody Carlumab (HY-P99188) conjugated to the protective group maleimidocaproyl and the tubulin inhibitor MMAF (HY-15579). The ADC toxic molecule and linker part are McMMAF (HY-15578). Anti-CCL2 (Carlumab)-McMMAF induces apoptosis and can be used in cancer research.
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PF-4178903
0 ImagesCat. No.: HY-119658CAS No.: 1310796-72-5Synonyms: INCB10820
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LUF7996
0 ImagesCat. No.: HY-180571CAS No.: 3104736-80-0LUF7996 is a CCR2 PROTAC Degrader degrading CCR2 with DC50 = 2.6 μM. LUF7996 demonstrates engagement of both and the E3 ligase cereblon and displays sustain and concentration-dependent degradation of CCR2. LUF7996 reliance on the lysosomal pathway to induce CCR2 degradation. LUF7996 efficiently inhibits monocyte migration in virto.
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CCR2 antagonist 6
0 ImagesCat. No.: HY-185299CAS No.: 1421063-89-9CCR2 antagonist 6 (Example 98) is a CCR2 antagonist (Kb: 0.215 μM for CCR2, 0.174 μM for hCCR2B). CCR2 antagonist 6 can be used in the research of inflammation and autoimmune diseases.
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Emapticap pegol scramble negative control
0 ImagesCat. No.: HY-148100CEmapticap pegol scramble negative control, an oligonucleotide aptamer, is the negative control of Emapticap pegol (HY-148100).
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CCR2 ligand-2
0 ImagesCat. No.: HY-D3598CAS No.: 2880299-29-4CCR2 ligand-2 is a small-molecule fluorescent ligand targeting the intracellular allosteric binding site (IABS) of CCR2, with a Kd value of 266 nM for membrane-based binding affinity and a Kd value of 114 nM for binding affinity in live cells. CCR2 ligand-2 enables non-isotopic, high-throughput cell-free and cell-based NanoBRET binding assays. CCR2 ligand-2 serves as a tool for fragment-based screening strategies.
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Anti-Mouse CCR2 Antibody (C2Mab-6)
0 ImagesCat. No.: HY-P991745Anti-Mouse CCR2 Antibody (C2Mab-6) is a monoclonal antibody targeting mouse CC chemokine receptor type 2 (mCCR2), with a KD value of 0.18-1.6 nM. Anti-Mouse CCR2 Antibody (C2Mab-6) exhibits high binding affinity to cells expressing mCCR2 and shows no reactivity to parental CHO-K1 cells. Anti-Mouse CCR2 Antibody (C2Mab-6) recognizes the amino acid region spanning positions 1-19 of mCCR2, and its key binding epitope includes Asp3, Asn4, Met6, Pro8, Gln9 and Phe10. Anti-Mouse CCR2 Antibody (C2Mab-6) can be used in leukemia-related research.
