Lfc Activators
Rho guanine nucleotide exchange factor 2 (ARHGEF2) activators comprise a diverse array of chemical compounds that enhance ARHGEF2's ability to facilitate the exchange of GDP for GTP on RhoA, thereby activating this GTPase and influencing various cellular processes such as cytoskeletal dynamics, cell migration, and proliferation. Y-27632 and Fasudil are both inhibitors of Rho-associated kinase (ROCK), and their activity can lead to an increase in ARHGEF2-mediated RhoA activation by alleviating the negative feedback inhibition on ARHGEF2. Similarly, NSC23766 acts by selectively inhibiting the interaction between Rac1 and its GEFs, thereby indirectly augmenting ARHGEF2's specificity for RhoA. Rho guanine nucleotide exchange factor 2 (ARHGEF2) activators are an ensemble of chemical entities that facilitate the activation of ARHGEF2, an exchange factor that catalyzes the GDP-GTP exchange on RhoA, a key regulator in cell signaling pathways.
The selective inhibition of ROCK by compounds like Y-27632 and Fasudil leads to the enhancement of ARHGEF2 activity by relieving the negative feedback on RhoA signaling, thereby increasing RhoA-mediated cellular responses. The action of NSC23766, which inhibits Rac1-GEF interaction, indirectly upregulates ARHGEF2 activity by reducing the availability of GEFs for Rac1, allowing more GEFs to interact with RhoA. The activation of RhoA signaling by lysophosphatidic acid and sphingosine-1-phosphate (S1P), through G-protein coupled receptor pathways, further supports the activation role of ARHGEF2 by enhancing its substrate availability. Furthermore, the non-hydrolyzable GTP analog, GTPγS, by stabilizing active G-protein forms, also enhances the exchange activity of ARHGEF2. The modulation of ARHGEF2 activity extends to the bacterial toxin CNF1, which activates Rho GTPases and thus indirectly augments ARHGEF2's functional role by increasing the pool of active RhoA. Statins, through the inhibition of HMG-CoA reductase, lead to reduced prenylation and membrane association of RhoA, enhancing the cytosolic activity of ARHGEF2.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $186.00 $707.00 | 88 | |
A selective inhibitor of ROCK, which in turn is a downstream effector of Rho proteins. Inhibition of ROCK leads to the activation of Rho guanine nucleotide exchange factor 2 (ARHGEF2) by relieving negative feedback loops, thus enhancing its GEF activity towards RhoA. | ||||||
NSC 23766 | 733767-34-5 | sc-204823 sc-204823A | 10 mg 50 mg | $151.00 $609.00 | 75 | |
Selectively inhibits Rac1-GEF interaction without affecting Cdc42 or RhoA. Augments ARHGEF2-mediated RhoA activation due to reduced competition from Rac1 for GEFs. | ||||||
(S)-(−)-Blebbistatin | 856925-71-8 | sc-204253 sc-204253A sc-204253B sc-204253C | 1 mg 5 mg 10 mg 25 mg | $72.00 $265.00 $495.00 $968.00 | ||
Functions as a bioactive lipid that activates RhoA through GPCR signaling which in turn stimulates Rho guanine nucleotide exchange factor 2 to enhance its exchange activity on RhoA. | ||||||
Guanosine 5′-O-(3-thiotriphosphate) tetralithium salt | 94825-44-2 | sc-202639 | 10 mg | $465.00 | ||
A non-hydrolyzable GTP analog that binds to and stabilizes the active forms of G proteins, thus potentiating ARHGEF2-induced RhoA activation. | ||||||
D-erythro-Sphingosine-1-phosphate | 26993-30-6 | sc-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 | |
Sphingosine-1-phosphate, a ligand for S1P receptors, which can activate RhoA GTPases through GPCR signaling, thereby increasing ARHGEF2 activity. | ||||||
Simvastatin | 79902-63-9 | sc-200829 sc-200829A sc-200829B sc-200829C | 50 mg 250 mg 1 g 5 g | $31.00 $89.00 $135.00 $443.00 | 13 | |
Inhibits HMG-CoA reductase leading to reduced isoprenylation and therefore reduced membrane association of RhoA, which may enhance cytosolic ARHGEF2 activity. | ||||||
EHop-016 | 1380432-32-5 | sc-497382 | 5 mg | $80.00 | ||
A Rac1 inhibitor that indirectly potentiates RhoA-ARHGEF2 signaling by decreasing the competitive binding of Rac1 to shared GEFs. | ||||||
Gallein | 2103-64-2 | sc-202631 | 50 mg | $85.00 | 20 | |
Blocks Gβγ signaling and can enhance ARHGEF2-mediated RhoA activation by disinhibiting GEFs that are normally sequestered by Gβγ subunits. | ||||||
ITX 3 | 347323-96-0 | sc-295214 sc-295214A | 10 mg 50 mg | $145.00 $615.00 | ||
An inhibitor of Trio, another GEF for Rho GTPases, potentially increasing the availability of RhoA for activation by ARHGEF2. | ||||||