Date published: 2026-3-11

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LGR5 Inhibitors

Common LGR5 Inhibitors include, but are not limited to Salinomycin CAS 53003-10-4, LGK 974 CAS 1243244-14-5, IWP-2 CAS 686770-61-6, Cercosporin CAS 35082-49-6 and Wnt-C59 CAS 1243243-89-1.

LGR5 inhibitors belong to a distinctive chemical class known for their ability to modulate the activity of the leucine-rich repeat-containing G protein-coupled receptor 5 (LGR5). These inhibitors operate by interfering with the interactions involving LGR5, a cell surface receptor that is often associated with stem cells in various tissues, including the gastrointestinal tract, hair follicles, and other regenerative niches. LGR5 plays a significant role in regulating stem cell self-renewal, proliferation, and differentiation, contributing to tissue maintenance and repair. LGR5 inhibitors are carefully designed to target specific binding sites or molecular pathways associated with LGR5, thereby influencing its cellular functions and downstream effects.

The development of LGR5 inhibitors requires a comprehensive understanding of the structural attributes of LGR5 and its interactions with its ligands. Researchers in this field work to engineer molecules with optimal selectivity and affinity for LGR5, enabling precise modulation of its activities. These inhibitors often incorporate innovative design strategies that disrupt key molecular interactions essential for LGR5's biological functions. By gaining insights into the intricate mechanisms through which LGR5 participates in various cellular processes, researchers aim to unravel its role in fundamental tissue regeneration and homeostasis. The continuous advancements in molecular biology and chemical synthesis drive the refinement of LGR5 inhibitors, holding promise for applications across diverse scientific contexts where manipulation of LGR5-mediated processes is of interest.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Salinomycin

53003-10-4sc-253530
sc-253530C
sc-253530A
sc-253530B
5 mg
10 mg
25 mg
100 mg
$162.00
$241.00
$406.00
$474.00
1
(1)

Selectively targets cancer stem cells by inhibiting Wnt signaling, including LGR5, leading to reduced proliferation and self-renewal of cancer stem cells.

LGK 974

1243244-14-5sc-489380
sc-489380A
5 mg
50 mg
$359.00
$1295.00
2
(0)

Porcupine inhibitor that interferes with Wnt secretion, blocking the activation of Wnt signaling pathway and affecting LGR5 expression and function.

IWP-2

686770-61-6sc-252928
sc-252928A
5 mg
25 mg
$96.00
$292.00
27
(1)

Disrupts Wnt protein secretion by inhibiting the acyltransferase Porcupine, leading to inhibition of LGR5-mediated Wnt signaling pathway.

PRI-724

1422253-38-0sc-507535
25 mg
$260.00
(0)

Inhibits CBP/beta-catenin interaction, reducing Wnt-mediated gene transcription and affecting LGR5 expression and downstream effects.

Cercosporin

35082-49-6sc-255013
5 mg
$459.00
1
(0)

Disrupts Wnt secretion by inhibiting Porcupine, resulting in reduced Wnt signaling activity and affecting LGR5-positive stem cells.

Wnt-C59

1243243-89-1sc-475634
sc-475634A
sc-475634B
5 mg
10 mg
50 mg
$214.00
$326.00
$1275.00
1
(0)

Inhibits the enzyme porcupine, necessary for Wnt acylation and secretion, leading to impaired Wnt signaling pathway and LGR5 expression.

XAV939

284028-89-3sc-296704
sc-296704A
sc-296704B
1 mg
5 mg
50 mg
$36.00
$117.00
$525.00
26
(1)

Stabilizes Axin protein and promotes beta-catenin degradation, leading to suppression of Wnt signaling pathway and LGR5 expression.

ETC-159

1638250-96-0sc-507415
5 mg
$90.00
(0)

Inhibits the enzyme Porcupine, responsible for Wnt palmitoylation and secretion, resulting in reduced LGR5-mediated Wnt signaling pathway activation.