EPI64 Inhibitors
Chemical inhibitors of EPI64 can impact its function through various mechanisms that involve the modulation of GTPase activities and actin cytoskeleton dynamics. NSC23766 disrupts the interaction between EPI64 and Rac1 by targeting Rac1's guanine nucleotide exchange factor activity, thus preventing the actin cytoskeleton reorganization where EPI64 is active. The importance of this interaction is further highlighted by compounds like EHop-016, which also targets the Rac1 GTPase pathway. EHop-016 inhibits the interaction between Vav2 and Rac1, reducing Rac1 activation, and consequently, the functionality of EPI64 in actin remodeling.
In the context of Cdc42 GTPase, which is a significant modulator of actin polymerization, ML141 and CASIN serve as inhibitors. ML141 selectively inhibits Cdc42, leading to downstream effects that include the impairment of actin remodeling processes where EPI64 is involved. CASIN also targets Cdc42, impacting EPI64's ability to influence cell shape and the actin cytoskeleton. ITX3, a selective Trio inhibitor, reduces the activity of Rac1 and RhoG GTPases, leading to decreased EPI64 activity in regulating the cytoskeleton and membrane trafficking. SecinH3 targets Cytohesin, which activates Arf GTPases involved in vesicular trafficking processes that EPI64 regulates, indicating that Cytohesin inhibition can restrain EPI64's regulatory capacity. Compounds like CID2950007 and Toxoflavin inhibit kinases and proteins that are crucial in the signaling pathways EPI64 is part of. CID2950007 directly inhibits PAK1, a kinase phosphorylating proteins involved in actin polymerization where EPI64 operates. Toxoflavin prevents Rac1 from binding to its GEFs, reducing Rac1 activation and therefore EPI64's associated functions. EHT 1864 destabilizes Rac-GTP binding and inhibits Rac-mediated signaling, which is essential for EPI64's role in regulating the actin cytoskeleton. Lastly, SMIFH2 inhibits formin-mediated actin assembly; since EPI64 is involved in actin dynamics, the suppression of formin activity can directly inhibit EPI64's function in maintaining the structure of the actin cytoskeleton.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
NSC 23766 | 733767-34-5 | sc-204823 sc-204823A | 10 mg 50 mg | $151.00 $609.00 | 75 | |
NSC23766 disrupts the interaction between EPI64 and the Rac1 GTPase by specifically targeting and inhibiting the Rac1-specific guanine nucleotide exchange factor (GEF) activity, thus functionally inhibiting EPI64's role in actin cytoskeleton reorganization. | ||||||
EHop-016 | 1380432-32-5 | sc-497382 | 5 mg | $80.00 | ||
EHop-016 acts by inhibiting the Vav2-Rac1 interaction, resulting in decreased Rac1 activation. By doing so, it functionally inhibits EPI64 since EPI64 modulates membrane trafficking and Rac1-dependent actin cytoskeleton changes. | ||||||
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 GTPase, an upstream regulator of actin polymerization processes. Inhibition of Cdc42 can lead to impaired actin remodeling, which is a process that EPI64 is known to influence, thereby functionally inhibiting EPI64. | ||||||
CASIN | 425399-05-9 | sc-397016 | 10 mg | $460.00 | 1 | |
CASIN inhibits the Cdc42 GTPase, which impacts actin polymerization and cell shape. Since EPI64 influences actin cytoskeleton configuration, its functional role is inhibited when Cdc42 activity is suppressed. | ||||||
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 for Rac1 and RhoG, which are GTPases involved in the regulation of actin dynamics. Inhibition of Trio leads to reduced EPI64 activity in the regulation of actin cytoskeleton and membrane trafficking. | ||||||
SecinH3 | 853625-60-2 | sc-203260 | 5 mg | $278.00 | 6 | |
SecinH3 inhibits Cytohesin, a GEF that activates Arf GTPases, which are implicated in vesicular trafficking processes that EPI64 is known to regulate. Thus, SecinH3 can functionally inhibit EPI64 by impacting these trafficking pathways. | ||||||
EHT 1864 | 754240-09-0 | sc-361175 sc-361175A | 10 mg 50 mg | $213.00 $889.00 | 12 | |
EHT 1864 is a Rac family small GTPase inhibitor that destabilizes Rac-GTP binding and inhibits Rac-mediated signaling pathways. This results in the functional inhibition of EPI64, which operates within these pathways to regulate actin cytoskeleton. | ||||||
SMIFH2 | 340316-62-3 | sc-507273 | 5 mg | $140.00 | ||
SMIFH2 is a small molecule inhibitor of formin-mediated actin assembly, which is crucial for maintaining actin structure. EPI64, which is involved in actin dynamics, is functionally inhibited when formin activity is suppressed. | ||||||