Date published: 2025-12-24

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CXCR-4 Inhibitors

CXCR-4, also known as CXC chemokine receptor 4, is a G protein-coupled receptor primarily recognized for its involvement in chemotaxis, or the directed migration of cells in response to a gradient of extracellular signaling molecules. This receptor is ubiquitously expressed on the surfaces of various cells, including hematopoietic stem cells, leukocytes, and endothelial cells, among others. CXCR-4's primary ligand is the chemokine CXCL12 (also known as stromal cell-derived factor-1 or SDF-1). When CXCL12 binds to CXCR-4, it triggers a cascade of intracellular events that can lead to various cellular responses, such as cell migration, proliferation, and survival. The CXCR-4/CXCL12 signaling axis plays a pivotal role in numerous physiological processes, including embryonic development, immune system function, and vascularization. CXCR-4 inhibitors are a class of compounds designed to modulate the activity of the CXCR-4 receptor. These inhibitors primarily operate by blocking the binding of CXCL12 to CXCR-4, thus preventing the activation of downstream signaling pathways. The molecular structures and mechanisms of action of these inhibitors can vary. Some might directly bind to the receptor's ligand-binding domain, obstructing the association with CXCL12. Others might alter the receptor's conformation, rendering it inactive. Additionally, some inhibitors might target and interfere with the intracellular components of the CXCR-4 signaling cascade. Given the diverse roles of the CXCR-4/CXCL12 axis in numerous biological processes, the study of CXCR-4 inhibitors offers insights into chemotaxis, cell signaling, and the intricacies of receptor-ligand interactions.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

AMD3100 octahydrochloride

155148-31-5sc-252367
5 mg
$90.00
19
(1)

AMD3100, also known as Plerixafor, is a known antagonist of CXCR-4 and can potentially down-regulate its expression in certain cells.

AMD 3465 hexahydrobromide

185991-07-5sc-362709
sc-362709A
10 mg
50 mg
$185.00
$772.00
(0)

AMD 3465 hexahydrobromide acts as a potent CXCR-4 antagonist, showcasing remarkable affinity for the receptor through specific ionic interactions and hydrophobic contacts. Its unique stereochemistry promotes conformational flexibility, allowing it to effectively disrupt receptor dimerization and downstream signaling cascades. The compound's high solubility in polar solvents enhances its bioavailability, while its bromide substituents introduce distinctive reactivity, influencing its behavior in diverse biochemical contexts.

TC 14012

368874-34-4sc-362800
sc-362800A
sc-362800B
1 mg
50 mg
100 mg
$199.00
$7500.00
$13500.00
(0)

TC 14012 functions as a selective CXCR-4 modulator, characterized by its ability to engage in specific hydrogen bonding and π-π stacking interactions with the receptor. This compound exhibits a unique conformational rigidity that stabilizes its binding, effectively inhibiting receptor activation. Its distinct electronic properties facilitate rapid reaction kinetics, while its solubility profile allows for versatile interactions in various biochemical environments, enhancing its functional versatility.

WZ811

55778-02-4sc-296701
sc-296701A
1 mg
5 mg
$29.00
$66.00
(0)

WZ811 is an effective CXCR-4 antagonist that might lead to receptor down-regulation by blocking its activation.

FC 131

606968-52-9sc-362738
1 mg
$430.00
(0)

FC-131 is a CXCR-4 antagonist, which can potentially down-regulate the receptor in certain cell types.

Plumbagin

481-42-5sc-253283
sc-253283A
100 mg
250 mg
$51.00
$61.00
6
(1)

Plumbagin acts as a CXCR-4 modulator, showcasing a unique ability to form strong hydrophobic interactions and coordinate bonds with the receptor. Its planar structure promotes effective π-π interactions, enhancing binding affinity. The compound's dynamic conformational flexibility allows it to adapt to different receptor states, influencing downstream signaling pathways. Additionally, its lipophilic nature contributes to its distribution in cellular membranes, impacting its interaction dynamics within complex biological systems.

MSX-122

897657-95-3sc-507328
50 mg
$690.00
(0)

MSX-122 is a partial CXCR-4 antagonist that can potentially reduce CXCR-4 levels in specific cells.

Gambogic Acid

2752-65-0sc-200137
sc-200137A
sc-200137B
sc-200137C
sc-200137D
5 mg
25 mg
100 mg
500 mg
1 g
$85.00
$243.00
$419.00
$720.00
$1230.00
5
(1)

Gambogic Acid has been shown to down-regulate CXCR-4 expression, potentially reducing tumor metastasis.

SR 48692

146362-70-1sc-363290
sc-363290A
sc-363290B
sc-363290C
sc-363290D
5 mg
25 mg
100 mg
500 mg
1 g
$156.00
$593.00
$2327.00
$10500.00
$20990.00
2
(0)

SR 48692 is an antagonist of CXCR-4 that might reduce its levels in specific cells.