Date published: 2026-5-16

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ARHGEF5L Activators

ARHGEF5L activators are a chemical class of compounds that target and modulate the activity of the ARHGEF5-like (ARHGEF5L) protein, which is a member of the Rho guanine nucleotide exchange factor (GEF) family. These activators play a pivotal role in the biochemical pathway by facilitating the exchange of GDP for GTP on Rho family GTPases, a process that is essential for the activation of these GTPases. The ARHGEF5L protein specifically is involved in the regulation of the actin cytoskeleton, which is crucial for a variety of cellular processes, including cell shape, migration, and division. The activators of this protein influence its ability to interact with Rho GTPases, thereby indirectly impacting the actin cytoskeletal dynamics and related cellular functions.

The molecular design of ARHGEF5L activators is focused on the enhancement of the guanine nucleotide exchange activity of the ARHGEF5L protein. By increasing the GEF activity, these compounds effectively facilitate the downstream signaling pathways that are regulated by the Rho GTPases. The activators themselves are diverse in structure, with each exhibiting a specific affinity and efficacy towards the ARHGEF5L protein. The interaction between the ARHGEF5L activators and the protein is governed by the structural complementarity, which determines the binding strength and the subsequent activation potency. The precise modulation of ARHGEF5L activity by these activators is critical in maintaining the balance of Rho GTPase-mediated signaling, which, in turn, has a significant impact on the cellular architecture and function. As such, the ARHGEF5L activators represent an important chemical class for the modulation of intracellular signaling pathways related to the cytoskeletal organization.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Forskolin

66575-29-9sc-3562
sc-3562A
sc-3562B
sc-3562C
sc-3562D
5 mg
50 mg
1 g
2 g
5 g
$78.00
$153.00
$740.00
$1413.00
$2091.00
73
(3)

Forskolin activates adenylate cyclase, increasing intracellular cAMP levels. Elevated cAMP activates PKA, which can then phosphorylate and activate ARHGEF5L, enhancing its guanine nucleotide exchange factor (GEF) activity towards its substrates.

Y-27632, free base

146986-50-7sc-3536
sc-3536A
5 mg
50 mg
$186.00
$707.00
88
(1)

Y-27632 is a ROCK inhibitor which leads to the activation of Rho GTPases. By inhibiting ROCK, Y-27632 indirectly activates ARHGEF5L by reducing the inhibitory phosphorylation events on downstream targets that would otherwise suppress ARHGEF5L's GEF activity.

EHT 1864

754240-09-0sc-361175
sc-361175A
10 mg
50 mg
$213.00
$889.00
12
(2)

EHT 1864 is a Rac1 inhibitor that stabilizes Rac1 in an inactive state. This can enhance ARHGEF5L activity by preventing Rac1 activation by other GEFs, thus increasing the availability of GTPases for ARHGEF5L-mediated activation.

Lysophosphatidic Acid

325465-93-8sc-201053
sc-201053A
5 mg
25 mg
$98.00
$341.00
50
(3)

Lysophosphatidic acid (LPA) is a bioactive lipid that activates Rho GTPases through G protein-coupled receptors. LPA signaling can enhance ARHGEF5L activity by promoting its GEF function towards Rho GTPases involved in cytoskeletal dynamics.

D-erythro-Sphingosine-1-phosphate

26993-30-6sc-201383
sc-201383D
sc-201383A
sc-201383B
sc-201383C
1 mg
2 mg
5 mg
10 mg
25 mg
$165.00
$322.00
$570.00
$907.00
$1727.00
7
(1)

Sphingosine 1-phosphate (S1P) acts via G protein-coupled receptors to activate Rho GTPases. S1P receptor signaling can enhance ARHGEF5L activity by promoting the GEF-mediated exchange of GDP for GTP on Rho GTPases.

Calpeptin

117591-20-5sc-202516
sc-202516A
10 mg
50 mg
$121.00
$456.00
28
(1)

Calpeptin is a calpain inhibitor which can prevent the cleavage and inactivation of GEFs. By protecting ARHGEF5L from calpain-mediated degradation, Calpeptin indirectly enhances the stability and activity of ARHGEF5L.

8-CPT-cAMP

93882-12-3sc-201569
sc-201569A
20 mg
100 mg
$87.00
$316.00
19
(1)

8-(4-Chlorophenylthio)-adenosine-3',5'-cyclic monophosphate (8-CPT-cAMP) is a cAMP analog that activates PKA. PKA can phosphorylate GEFs, potentially enhancing ARHGEF5L activity by increasing its interaction with Rho GTPases.