PLEKHG2 Inhibitors
Chemical inhibitors of PLEKHG2 function by targeting various proteins that interact with or regulate PLEKHG2, impacting its role in cellular signaling pathways. Y-27632 is one such inhibitor, which specifically inhibits ROCK, a kinase that is a downstream effector of Rho GTPases. By inhibiting ROCK, Y-27632 reduces the signaling cascades that PLEKHG2 may mediate. Similarly, NSC23766 targets Rac1, a small GTPase that directly interacts with PLEKHG2 to modulate its guanine nucleotide exchange factor (GEF) activity. Inhibition of Rac1 by NSC23766 can decrease the functional activation of PLEKHG2. ML141 and CASIN are selective inhibitors of Cdc42, another GTPase that influences PLEKHG2. By inhibiting Cdc42, these compounds can diminish PLEKHG2's role in the organization of the actin cytoskeleton.
Other inhibitors such as SecinH3 and ITX3 indirectly influence PLEKHG2 activity by targeting proteins with related functions. SecinH3 inhibits cytohesins, impacting ARF-mediated pathways that may intersect with PLEKHG2's pathways. ITX3, a selective inhibitor of Trio, can limit PLEKHG2's role by reducing the activity of Trio-regulated pathways. ZCL278, another Cdc42 GEF inhibitor, can reduce PLEKHG2 GEF activity by blocking the interaction between Cdc42 and its GEFs, including PLEKHG2. EHT 1864 directly inhibits Rac1 binding and activation, which leads to decreased PLEKHG2 activity. Similarly, Toxin B, a glucosyltransferase, inactivates Rho GTPases such as Rho, Rac, and Cdc42, which are upstream regulators of PLEKHG2, thus having an inhibitory effect on PLEKHG2 function. CID2950007 and IPA-3 both inhibit PAK1, a downstream effector of Rac1, which can diminish signaling pathways that involve PLEKHG2. Lastly, SMIFH2 inhibits formin homology 2 domain proteins, which are regulated by Rho GTPases, thus disrupting actin dynamics and indirectly inhibiting PLEKHG2 activity.
SEE ALSO...
| 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 | |
Y-27632 is a selective inhibitor of ROCK (Rho-associated protein kinase). PLEKHG2, as a Rho guanine nucleotide exchange factor (GEF), is activated by Rho GTPases. Inhibiting ROCK may reduce PLEKHG2-mediated downstream signaling. | ||||||
ML 141 | 71203-35-5 | sc-362768 sc-362768A | 5 mg 25 mg | $137.00 $512.00 | 7 | |
ML141 is a selective inhibitor of Cdc42, another GTPase that interacts with PLEKHG2. Cdc42 inhibition can lead to decreased PLEKHG2 GEF activity, thus inhibiting PLEKHG2 function in actin cytoskeleton organization. | ||||||
SecinH3 | 853625-60-2 | sc-203260 | 5 mg | $278.00 | 6 | |
SecinH3 targets cytohesins, which are GEFs for ADP-ribosylation factors (ARFs), indirectly influencing PLEKHG2 function by modulating ARF-mediated pathways that could be involved in the same cellular processes as PLEKHG2. | ||||||
CASIN | 425399-05-9 | sc-397016 | 10 mg | $460.00 | 1 | |
CASIN inhibits Cdc42 activity, and given that Cdc42 can regulate PLEKHG2, inhibition of Cdc42 by CASIN can result in reduced PLEKHG2-mediated signaling responsible for cellular processes such as migration and invasion. | ||||||
ITX 3 | 347323-96-0 | sc-295214 sc-295214A | 10 mg 50 mg | $145.00 $615.00 | ||
ITX3 is a selective inhibitor of Trio, a GEF protein that has overlapping functions with PLEKHG2. Inhibiting Trio can indirectly reduce PLEKHG2's role in Trio-regulated pathways, thus functionally inhibiting PLEKHG2. | ||||||
ZCL278 | 587841-73-4 | sc-507369 | 10 mg | $115.00 | ||
ZCL278 is a Cdc42 GEF inhibitor, and it can inhibit the interaction of Cdc42 with its GEFs, including PLEKHG2. This inhibition can reduce the GEF activity of PLEKHG2, diminishing its functional role in the cell. | ||||||
EHT 1864 | 754240-09-0 | sc-361175 sc-361175A | 10 mg 50 mg | $213.00 $889.00 | 12 | |
EHT 1864 is a Rac1 inhibitor, which directly inhibits Rac1 binding and activation. Since Rac1 is a known regulator of PLEKHG2, inhibiting Rac1 can lead to decreased activation of PLEKHG2, inhibiting its function. | ||||||
SMIFH2 | 340316-62-3 | sc-507273 | 5 mg | $140.00 | ||
SMIFH2 is an inhibitor of formin homology 2 (FH2) domain proteins, which are regulated by Rho GTPases. Inhibition of these proteins can indirectly inhibit PLEKHG2 by disrupting actin dynamics that PLEKHG2 is involved in regulating. | ||||||
IPA 3 | 42521-82-4 | sc-204016 sc-204016A | 5 mg 50 mg | $94.00 $458.00 | 6 | |
IPA-3 is a selective non-ATP competitive inhibitor of PAK1, an effector of Rac1 GTPase. By inhibiting PAK1, IPA-3 may diminish PLEKHG2 activity by reducing the influence of Rac1 on actin cytoskeletal changes and cellular signaling. | ||||||