Date published: 2026-4-10

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EDG-8 Inhibitors

EDG-8, also known as S1P receptor 5 (S1P5), is a G protein-coupled receptor (GPCR) that belongs to the endothelial differentiation gene (EDG) family. It is primarily expressed in various tissues, including the central nervous system, cardiovascular system, and immune cells. EDG-8 plays a crucial role in mediating cellular responses to sphingosine-1-phosphate (S1P), a bioactive lipid mediator involved in diverse physiological processes such as cell proliferation, migration, angiogenesis, immune cell trafficking, and vascular tone regulation. Activation of EDG-8 by S1P triggers downstream signaling cascades, including the activation of phospholipase C (PLC), phosphatidylinositol 3-kinase (PI3K), and extracellular signal-regulated kinase (ERK), leading to various cellular responses and functional outcomes. Inhibition of EDG-8 function represents a strategy for modulating S1P-mediated signaling pathways and associated physiological processes. Several mechanisms of inhibition have been proposed, including the development of small molecule antagonists or inverse agonists that bind to the receptor and block its activation by S1P. These antagonists can competitively inhibit S1P binding to EDG-8, thereby impeding downstream signaling events and cellular responses associated with receptor activation. Additionally, targeting downstream signaling components or effectors of EDG-8-mediated pathways may also represent alternative approaches for inhibiting the functional outcomes of EDG-8 activation. By elucidating the mechanisms of EDG-8 inhibition, researchers can gain insights into strategies for modulating S1P-mediated cellular responses and exploring the implications of targeting this receptor in various pathological conditions.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

SEW2871

256414-75-2sc-203251
sc-203251A
5 mg
10 mg
$38.00
$53.00
1
(0)

SEW2871 inhibits EDG-8 by specifically targeting the receptor and blocking its activation by sphingosine-1-phosphate (S1P). This inhibition disrupts the S1P signaling pathway, leading to downstream effects on cellular processes regulated by EDG-8, such as cell migration, proliferation, and survival.

PF-543

1415562-82-1sc-507507
10 mg
$210.00
(0)

PF-543 inhibits EDG-8 by targeting sphingosine kinase (SphK), the enzyme responsible for generating S1P. By blocking SphK, PF-543 disrupts the synthesis of S1P, preventing its interaction with EDG-8 and thereby inhibiting downstream signaling events associated with EDG-8 activation.

2-undecyl-thiazolidine-4-carboxylic acid

298186-80-8sc-220768
sc-220768A
5 mg
10 mg
$88.00
$166.00
(0)

Also called BML-241, this compound inhibits EDG-8 by acting as a selective antagonist, preventing the binding of S1P to the receptor. This antagonistic action disrupts the normal activation of EDG-8 by S1P, leading to alterations in the signaling cascades controlled by EDG-8 and influencing cellular responses such as migration, proliferation, and survival.

VPC 23019

449173-19-7sc-362817
10 mg
$364.00
4
(1)

VPC-23019 inhibits EDG-8 by specifically targeting the receptor and interfering with its coupling to G proteins. This disruption of the G protein-mediated signaling pathway prevents the downstream effects of EDG-8 activation, impacting cellular processes regulated by EDG-8, including cell migration, proliferation, and survival.

FTY720

162359-56-0sc-202161
sc-202161A
sc-202161B
1 mg
5 mg
25 mg
$33.00
$77.00
$120.00
14
(1)

FTY720 inhibits EDG-8 by acting as a functional antagonist, causing internalization and degradation of the receptor. This internalization prevents the activation of EDG-8 by S1P and disrupts downstream signaling events, influencing cellular processes like cell migration, proliferation, and survival regulated by EDG-8.

D-erythro-Sphingosine

123-78-4sc-3546
sc-3546A
sc-3546B
sc-3546C
sc-3546D
sc-3546E
10 mg
25 mg
100 mg
1 g
5 g
10 g
$90.00
$194.00
$510.00
$2448.00
$9384.00
$15300.00
2
(2)

Sphingosine inhibits EDG-8 by competitively binding to the receptor, preventing the activation of EDG-8 by S1P. This competitive inhibition disrupts the normal signaling cascade initiated by EDG-8 activation, leading to alterations in cellular processes such as cell migration, proliferation, and survival regulated by EDG-8.

W146

909725-61-7sc-507557
1 mg
$525.00
(0)

W146 inhibits EDG-8 by acting as a selective antagonist, preventing the binding of S1P to the receptor. This antagonistic action disrupts the normal activation of EDG-8 by S1P, leading to alterations in the signaling cascades controlled by EDG-8 and influencing cellular responses such as migration, proliferation, and survival.

JTE 013

383150-41-2sc-203615
10 mg
$195.00
5
(1)

JTE-013 inhibits EDG-8 by specifically targeting the receptor and blocking its activation by S1P. This inhibition disrupts the S1P signaling pathway, leading to downstream effects on cellular processes regulated by EDG-8, such as cell migration, proliferation, and survival.