CXCRs (CXC chemokine receptors) are membrane-integral proteins that bind and react to particular members of the CXC chemokine family of cytokines. They belong to a large family of G protein-linked receptors known as seven transmembrane (7-TM) proteins because they span the cell membrane seven times. They are one subfamily of chemokine receptors. CXCR1 through CXCR7 are the seven CXC chemokine receptors that are currently recognized in mammals.The CXC chemokine receptors CXCR1 and CXCR2 recognize CXC chemokines that have an E-L-R amino acid motif right next to their CXC motif. The majority of CXCR3-expressing cells are T lymphocytes. Like CCR5, CXCR4 is the receptor for a chemokine called CXCL12 (also known as SDF-1), and it is used by HIV-1 to enter target cells.The B cell-specific chemokine receptor CXCR5 plays a role in lymphocyte homing and the maturation of healthy lymphoid tissue. Prior to being given the name CXCR6, CXCR6 was known by three different names (STRL33, BONZO, and TYMSTR) because of its chromosomal location and similarity to other chemokine receptors in its gene sequence. CXCR7 was previously known as RDC-1 (an orphan receptor), but after it was discovered that CXCL12 (the ligand for CXCR4) causes chemotaxis in T lymphocytes, this molecule was renamed to CXCR7.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V78893 | CTCE-9908 TFA | CTCE-9908 TFA is a potent and specific CXCR4 inhibitor. | |
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V51660 | CXCR2 antagonist 2 | 2647464-91-1 | CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immune research with IC50 of 95 nM. |
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V51658 | CXCR2 antagonist 3 | 2647464-92-2 | CXCR2 Antagonist 3 (compound 11h) is a potent antagonist of CXC chemokine receptor 2 (CXCR2). |
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V3791 | CXCR2-IN-1 | 1873376-49-8 | CXCR2-IN-1 is a novel CNS (central nervous system) penetrant antagonist of CXCR2 with a pIC50 of 9.3. |
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V51654 | CXCR2-IN-2 | 1838123-21-9 | CXCR2 antagonist |
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V51657 | CXCR4 antagonist 1 | 675135-69-0 | CXCR4 antagonist 1 is a potent CXCR4 antagonist. |
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V51659 | CXCR4 antagonist 2 | 2243636-57-7 | CXCR4 antagonist 2 is a CXCR4 antagonist (inhibitor) with IC50 of 47 nM. |
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V51656 | CXCR4 antagonist 3 | 2761009-43-0 | CXCR4 Antagonist 3 (Compound 12a) is a potent CXCR4 antagonist (inhibitor) with IC50 of 11 nM. |
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V74888 | CXCR4 antagonist 4 | 2761009-30-5 | CXCR4 antagonist 4 is a potent, orally bioactive CXCR4 antagonist (IC50=24 nM), which can reduce the activity of CYP 2D6, increase the permeability of PAMPA, and effectively inhibit the entry of human immunodeficiency virus (IC50=7 nM) . |
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V51655 | CXCR4-IN-1 | 2304750-48-7 | CXCR4-IN-1 (Example C5) is a CXCR4 kinase (IC50= 20 nM). |
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V79685 | CXCR4-IN-2 | CXCR4-IN-2 (compound A1) is a bifunctional fluorinated small molecule, a potent CXCR4 inhibitor (antagonist) with anti-cancer activity. | |
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V51650 | CXCR7 antagonist-1 | 1613021-99-0 | CXCR7 antagonist |
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V51662 | CXCR7 modulator 1 | 2231812-31-8 | CXCR7 modulator 1 (compound 25) is an orally bioactive, peptidoid modulator of CXCR7 with Ki of 9 nM. |
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V51661 | CXCR7 modulator 2 | 2227426-37-9 | CXCR7 modulator 2 is a modulator of CXCR7 with Ki of 13 nM. |
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V3796 | Danirixin | 954126-98-8 | Danirixin (formerly known asGSK-1325756; GSK1325756) is a novel, potent small molecule CXCR2 antagonist being developed as a potential anti-inflammatory drug for COPD. |
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V51663 | DOTA-CXCR4-L | DOTA-CXCR4-L is a CXCR4-targeting peptide. | |
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V79235 | E70K | E70K is a CXCL8 C-terminal peptide in which glutamic acid replaces lysine at position 70. | |
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V51646 | Eldelumab (BMS-936557; MDX-1100) | 946414-98-8 | Eldelumab (BMS-936557) is a humanized anti-CXCL10 (IP-10) monoclonal antibody (mAb) (IgG1 type). |
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V52965 | FC131 TFA | 842166-42-1 | FC131 TFA is a CXCR4 antagonist that inhibits the binding of [125I]-SDF-1 to CXCR4 with an IC50 value of 4.5 nM. FC131 TFA has anti-HIV activity. |
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V13399 | IT1t dihydrochloride | 1092776-63-0 | IT1t is a novel, potent and selective CXCR4 antagonist with an IC50 of 1.1 nM in calcium mobilization assay, it can be potentially used as an anti-HIV agent. |
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