CXCR

CXCR

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.

CXCR related products

Structure Cat No. Product Name CAS No. Product Description
V51897 KRH-3955 hydrochloride 2253744-59-9 KRH-3955 hydrochloride is an orally active CXCR4 antagonist. KRH-3955 hydrochloride inhibits the binding of SDF-1α to CXCR4 with an IC50 of 0.61 nM.
V4031 LIT-927 2172879-52-4 LIT-927 (LIT927 ) is a novel potent, locally and orally bioactive neutraligand for the chemokine CXCL12 with anti-inflammatory and anticancer activity.
V4853 LY-2510924 1088715-84-7 LY2510924 (LY-2510924),a small cyclicpeptide, is a novel, potent and selective CXCR4 (CXC chemokine receptor 4) antagonist with potential anticancer and anti-inflammatory activity.
V3260 Mavorixafor (AMD-070) 558447-26-0 Mavorixafor (AMD-070; AMD11070, AMD070, X4P-001) is an orally bioavailable CXCR4 antagonist with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, it inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.
V51808 Mavorixafor trihydrochloride (AMD-070 trihydrochloride) 2309699-17-8 Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective, orally available CXCR4 antagonist that can antagonize the binding of 125I-SDF to CXCR4 with an IC50 value of 13 nM.
V51651 Minecoside 51005-44-8 Minecoside is a CXCR4/STAT3 activator with anti-cancer and anti-inflammatory activities.
V25675 ML-339 2080300-49-6 ML-339 is a novel and potent hCXCR6 antagonist (IC50 of 140 nM) with anticancer activity and selectivity (IC50 >79 μM) against CXCR5, CXCR4, CCR6 and Apelin receptor (APJ).
V20632 MSX-122 897657-95-3 MSX-122 is a novel, potent and orally bioavailable inhibitor/partial antagonist of CXCR4 which inhibits CXCR4/CXCL12 actions with an IC50 of 10 nM.
V26716 MSX-127 (NSC-23026) 6616-56-4 MSX-127 is a CXCR4 antagonist.
V26051 MSX-130 4051-59-6 MSX-130 is a CXCR4 antagonist.
V3792 Navarixin 473727-83-2 Navarixin (formerly known as MK-7123; SCH527123; PS291822) is a novel potent and specific allosteric antagonist of CXCR1 and CXCR2 with antitumor and anti-inflammatory activity and is able to sensitize cells to oxaliplatin in preclinical colon cancer models.
V5173 NBI-74330 855527-92-3 NBI-74330 (NBI74330) is a novel, potent and selective antagonist for CXCR3 (CXC chemokine receptor 3) with potential anticancer, immunomodulatory and antiinflammatory activities.
V51675 NoxaBH3 NoxaBH3 is a cysteine-based cross-linked peptide with increased cell permeability and higher inhibitory activity against Mcl-1.
V38879 NUCC-390 diHCl NUCC-390diHCl is a novel, potent, and specific small-molecule CXCR4 receptor agonist.
V74887 NUCC-390 dihydrochloride 2749281-71-6 NUCC-390 di-HCl is a new type of selective small molecule CXCR4 receptor agonist.
V74883 Olaptesed pegol 1390628-22-4 Olaptesed pegol (NOX-A12) L-oligoribonucleotide aptamer targeting CXCL12 based on pegylated structure.
V81002 Olaptesed pegol sodium Olaptesed pegol sodium is a CXCL12-targeting L-oligoribonucleotide aptamer based on a pegylated structure.
V51672 Peptide R 1774344-28-3 Peptide R is a gap peptide and a CXCR4 antagonist.
V1488 Plerixafor (AMD 3100) 110078-46-1 Plerixafor (formerly known as SDZ-SID-791; JLK-169; SID-791;AMD3100, AMD-3100, JM-3100, JM 3100; trade name Mozobil), the so called hematopoeitic stem cell mobilizer,is a novel and potent chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with an IC50 of 44 nM and 5.7 nM in cell-free assays, respectively.
V1487 Plerixafor 8HCl (AMD3100) 155148-31-5 Plerixafor 8HCl (formerly JM-3100; AMD-3100; SDZ-SID-791; JLK-169; SID-791; JM-2987; MOZOBIL), the hydrochloride salt of Plerixafor, is a specific chemokine receptor CXCR4 antagonist used as an immunostimulant to mobilize hematopoietic stem cells in cancer patients into the bloodstream.
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