PDZ-RhoGEF Activators
The chemical class of PDZ-RhoGEF Activators represents a group of compounds that indirectly stimulate the activity of PDZ-RhoGEF, a protein involved in Rho GTPase signaling and the regulation of the actin cytoskeleton. These activators do not directly interact with PDZ-RhoGEF but exert their effects by modulating key components and pathways related to its function. This class is characterized by its diversity, including various inhibitors of ROCK, Rac1, Cdc42, and other molecules involved in Rho GTPase signaling and cytoskeletal dynamics. The indirect activation of PDZ-RhoGEF by these compounds is achieved through altering the balance and dynamics of Rho GTPase signaling, which is central to PDZ-RhoGEF's regulatory role in the cell.
The mechanisms of action of these inhibitors are complex and multifaceted, reflecting the intricacy of the signaling networks in which PDZ-RhoGEF operates. For instance, ROCK inhibitors like Y-27632 and Fasudil modulate the actin cytoskeleton by influencing downstream Rho GTPase signaling, thereby potentially affecting PDZ-RhoGEF activity. Similarly, inhibitors of Rac1 (such as NSC23766 and EHT 1864) and Cdc42 (like ML141 and CASIN) target specific members of the Rho GTPase family, thereby influencing the overall signaling network and indirectly modulating PDZ-RhoGEF activity. Other compounds, such as Rhosin and ITX3, act on the interaction between Rho GTPases and their GEFs, further demonstrating the diverse approaches to modulating PDZ-RhoGEF activity.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $182.00 $693.00 | 88 | |
A ROCK inhibitor, Y-27632 relaxes the actin cytoskeleton by inhibiting ROCK, which can indirectly activate PDZ-RhoGEF by altering Rho GTPase signaling, a pathway in which PDZ-RhoGEF is involved. | ||||||
CCG-1423 | 285986-88-1 | sc-205241 sc-205241A | 1 mg 5 mg | $30.00 $90.00 | 8 | |
CCG-1423 inhibits RhoA-mediated gene transcription. This inhibition could alter the cellular environment in a way that indirectly activates PDZ-RhoGEF by modulating Rho GTPase signaling pathways. | ||||||
NSC 23766 | 733767-34-5 | sc-204823 sc-204823A | 10 mg 50 mg | $148.00 $597.00 | 75 | |
NSC23766 inhibits Rac1, a Rho GTPase family member. By inhibiting Rac1, it can influence Rho GTPase signaling balance, potentially leading to the activation of PDZ-RhoGEF. | ||||||
ML 141 | 71203-35-5 | sc-362768 sc-362768A | 5 mg 25 mg | $134.00 $502.00 | 7 | |
ML141 is a Cdc42 inhibitor. Inhibition of Cdc42, another Rho GTPase, can affect the overall Rho GTPase signaling balance, potentially leading to indirect activation of PDZ-RhoGEF. | ||||||
Rhosin | 1173671-63-0 | sc-507401 | 25 mg | $555.00 | ||
Rhosin is a direct inhibitor of RhoA binding to GEFs. By inhibiting this interaction, Rhosin can modulate the downstream signaling and potentially indirectly activate PDZ-RhoGEF by altering Rho GTPase dynamics. | ||||||
EHT 1864 | 754240-09-0 | sc-361175 sc-361175A | 10 mg 50 mg | $209.00 $872.00 | 12 | |
EHT 1864 is a Rac1 inhibitor. Its action on Rac1 can indirectly influence PDZ-RhoGEF activity by modulating the Rho GTPase signaling network. | ||||||
CASIN | 425399-05-9 | sc-397016 | 10 mg | $460.00 | 1 | |
CASIN inhibits Cdc42. This inhibition can affect cell cytoskeleton dynamics and Rho GTPase signaling pathways, potentially leading to the indirect activation of PDZ-RhoGEF. | ||||||
ITX 3 | 347323-96-0 | sc-295214 sc-295214A | 10 mg 50 mg | $145.00 $615.00 | ||
ITX3 is a specific inhibitor of Trio, a guanine nucleotide exchange factor for Rac1 and RhoG. By inhibiting Trio, ITX3 can modulate Rho GTPase signaling, potentially leading to the indirect activation of PDZ-RhoGEF. | ||||||
Fasudil, Monohydrochloride Salt | 105628-07-7 | sc-203418 sc-203418A sc-203418B sc-203418C sc-203418D sc-203418E sc-203418F | 10 mg 50 mg 250 mg 1 g 2 g 5 g 10 g | $18.00 $32.00 $85.00 $165.00 $248.00 $486.00 $910.00 | 5 | |
Fasudil is a ROCK inhibitor. Similar to Y-27632, it modulates Rho GTPase signaling by inhibiting ROCK, potentially leading to the indirect activation of PDZ-RhoGEF through altered cytoskeletal dynamics. | ||||||
SMIFH2 | 340316-62-3 | sc-507273 | 5 mg | $140.00 | ||
SMIFH2 inhibits formin-mediated actin assembly. Since formins are downstream effectors of Rho GTPases, their inhibition can alter cytoskeletal dynamics and indirectly influence PDZ-RhoGEF activity. | ||||||