cxcr4

Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.

Plerixafor octahydrochloride (JM3100 octahydrochloride) blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation. Plerixafor is a bicyclam with hematopoietic stem cell-mobilizing activity.

AMD-070 hydrochloride is a CXCR4 antagonist, is useful for Anti HIV.

ALX 40-4C acetate is a CXCR4 inhibitor of the chemokine receptor (Ki = 1 μM) and suppresses the replication of X4 strains of HIV-1. ALX 40-4C acetate is an antagonist of the APJ receptor (IC50 = 2.9 μM).

Mavorixafor (AMD-070) is an effective and selective antagonist of CXCR4, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. Mavorixafor inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells (IC50 = 1 nM) and PBMCs (IC50 = 9 nM).

CXCR4 antagonist 9 (Compound 2) is a potent CXCR4 antagonist with an IC50 of 15 nM and effectively inhibits the cytosolic calcium increase induced by CXCL12, exhibiting an IC50 of 1.3 nM [1].

CXCR4 antagonist 7 (Compound PARA-B) is a potent CXCR4 inhibitor (IC50 = 9.3 nM) [1] applicable in research on HIV infection, inflammatory diseases, cancer, and WHIM syndrome.

CXCR4 antagonist 3 (compound 12a), an effective antagonist of CXCR4, exhibits an IC50 of 11 nM. It is a congener of TIQ15, showcasing exceptional properties such as CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. With its potential for research on the human immunodeficiency virus, CXCR4 antagonist 3 holds great promise [1].

CXCR4 antagonist 8 (Compound 3) is a potent inhibitor of CXCR4, exhibiting an IC50 value of 57 nM in antagonism and effectively inhibiting CXCL12-induced cytosolic calcium increase with an IC50 of 0.24 nM. Additionally, Compound 3 is efficacious in inhibiting CXCL12 CXCR4-mediated cell migration [1].

CXCR4 antagonist 4 is an orally active and potent CXCR4 antagonist with an IC50 of 24 nM. CXCR4 antagonist 4 inhibits CYP 2D6 activity, increases PAMPA permeability, and effectively blocks entry of human immunodeficiency virus (IC50=7 nM).

CXCR4-IN-2 (compound A1), a potent bifunctional fluorinated small molecule, inhibits CXCR4 and exhibits anticancer properties by exerting cytotoxicity (IC 50: 60 μg mL; 72 h) and antiproliferative effects on mouse colorectal cancer (CRC) cells. It induces G2 M phase cell cycle arrest and apoptosis [1].

CXCR4 probe 1 (compound 5) is a potent and specific CXCR4-targeted PET tracer that acts on the CXCR4-specific antagonist TN14003 (IC50: 6.9 nM). It has potential as a CXCR4-specific imaging probe for the diagnosis and prognostic monitoring of inflammatory diseases, CXCR4-positive tumors, and metastatic tumors.

CXCR4 modulator-2 (compound Z7R) is a potent CXCR4 modulator with an IC50 of 1.25 nM, exhibits good stability in mouse serum (t1 2 = 77.1 min), and shows anti-inflammatory effects in a mouse oedema model.

CXCR4 antagonist10 (compound 21) is an effective CXCR4 inhibitor with an IC50 value of 7.8 nM. It plays a significant role in cancer research.

CXCR4 antagonist 1 is a potent inhibitor of the CXCR4 receptor with notable anti-HIV activity.

CXCR4 antagonist 6 (compound 46) is a highly potent inhibitor of CXCR4 with an IC50 value of 79 nM, effectively inhibiting the cytosolic calcium flux induced by CXCL12 with an IC50 of 0.25 nM. Additionally, it significantly mitigates cell migration mediated by the CXCL12 CXCR4 interaction and demonstrates remarkable efficacy in a mouse model of cancer metastasis [1].

CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator (EC50 = 100 nM) with research value in anti-inflammatory, anticancer, and anti-HIV studies.

CXCR4 antagonist 2 is a CXCR4 antagonist with an IC50 value of 47 nM.

DOTA-CXCR4-L, a peptide targeting the CXCR4 receptor, is utilized in cancer research, notably in the contexts of glioblastoma and triple-negative breast cancer [1].

CXCR4-IN-1 (Example C5), with an IC50 of 20 nM, is a potent inhibitor of CXCR4, applicable for the research of various conditions such as cancer, HIV, diabetic retinopathy, and inflammation [1].

CXCR4 antagonist 5 (compound 23), a potent CXCR4 antagonist, exhibits high inhibition efficacy against CXCR4 with an IC50 value of 8.8 nM. It effectively suppresses CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and hinders CXCR4 CXCL12-mediated chemotaxis. Moreover, Compound 23 demonstrates favorable physicochemical properties and in vitro safety profiles, exhibiting only marginal to moderate inhibition of CYP isozymes and hERG [1].

NUCC-390, a novel small-molecule CXCR4 receptor agonist, selectively induces CXCR4 receptor internalization while acting antagonistically to AMD3100. This compound facilitates nerve functional recovery following neurodegeneration in vivo.

Tannic acid (Gallotannic acid) is a novel hERG channel blocker.

Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent CXCR4 antagonist with anti-angiogenic properties, potentially valuable in treating choroid neovascularization.