ARHGAP11A Activators
ARHGAP11A activators are a class of chemical agents that specifically interact with the ARHGAP11A protein, a member of the Rho GTPase activating protein (GAP) family. ARHGAP11A is an intriguing protein that has been identified as playing a role in the modulation of the actin cytoskeleton. Rho GTPases are a subfamily of the Ras superfamily and are involved in various cellular processes, including the organization of the actin cytoskeleton, cell migration, cell proliferation, and cell cycle progression. The GAPs, such as ARHGAP11A, function by accelerating the hydrolysis of GTP bound to Rho proteins, thereby inactivating the Rho proteins and serving as negative regulators of the signaling pathways that they control. ARHGAP11A activators, therefore, influence the activity of ARHGAP11A, which in turn modifies the activity of Rho GTPases, ultimately affecting actin cytoskeleton dynamics.
From a biochemical perspective, ARHGAP11A activators would bind to the ARHGAP11A protein and enhance its GAP activity. This enhancement alters the intracellular balance of active and inactive Rho GTPases. The precise mechanism of how these activators function at the molecular level might involve allosteric modulation of the ARHGAP11A protein, leading to a conformational change that increases its affinity or catalytic efficiency towards its Rho GTPase substrates. The activators might achieve this by binding to a site distinct from the active site, a common method of action for allosteric effectors. The modulation of ARHGAP11A activity has the potential to impact various aspects of cellular dynamics, emphasizing the significance of these molecules in the intricate regulation of cellular processes that are fundamental to the maintenance of cellular structure and function. The study of ARHGAP11A activators is a vivid example of how small molecules can exert powerful effects on complex intracellular signaling pathways.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
PMA | 16561-29-8 | sc-3576 sc-3576A sc-3576B sc-3576C sc-3576D | 1 mg 5 mg 10 mg 25 mg 100 mg | $41.00 $132.00 $214.00 $500.00 $948.00 | 119 | |
PMA acts as a diacylglycerol analog to activate protein kinase C (PKC), which can lead to the downstream activation of small GTPases including Rho family proteins. ARHGAP11A, as a Rho GTPase activating protein, would have its GAP activity enhanced as part of the feedback regulation of Rho GTPases. | ||||||
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, a Rho-associated protein kinase. Inhibition of ROCK leads to increased GTP-bound RhoA, subsequently increasing the activity of ARHGAP11A as it acts to convert the active RhoA-GTP to its inactive GDP-bound state. | ||||||
NSC 23766 | 733767-34-5 | sc-204823 sc-204823A | 10 mg 50 mg | $151.00 $609.00 | 75 | |
NSC23766 inhibits the interaction between Rac1 and its GEFs, leading to a reduced level of active Rac1. This allows ARHGAP11A to enhance its activity towards inactivating Rac1 by promoting GTP hydrolysis. | ||||||
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. It prevents the activation of Cdc42, which could lead to an increased requirement for ARHGAP11A activity to maintain homeostasis of Cdc42 activity levels. | ||||||
EHop-016 | 1380432-32-5 | sc-497382 | 5 mg | $80.00 | ||
EHop-016 is a Rac1 inhibitor that binds to Vav2, preventing Rac1 activation. As ARHGAP11A is involved in inactivating Rac1, the presence of EHop-016 would enhance ARHGAP11A's GAP activity to shift the equilibrium towards the inactive form of Rac1. | ||||||
CASIN | 425399-05-9 | sc-397016 | 10 mg | $460.00 | 1 | |
CASIN inhibits the activation of Cdc42, which could lead to a compensatory increase in ARHGAP11A activity as the cell seeks to regulate the levels of active Cdc42. | ||||||
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 guanine nucleotide exchange factor (GEF) for Rac1 and RhoG. Inhibition of Trio would reduce the levels of GTP-bound Rac1 and RhoG, hence potentially enhancing the activity of ARHGAP11A in maintaining Rho GTPase activity balance. | ||||||
Rhosin | 1173671-63-0 | sc-507401 | 25 mg | $555.00 | ||
Rhosin specifically binds to RhoA and prevents its activation by GEFs. This could indirectly enhance the activity of ARHGAP11A by increasing the cellular demand for its GAP function to regulate the inactive state of RhoA. | ||||||
ZCL278 | 587841-73-4 | sc-507369 | 10 mg | $115.00 | ||
ZCL278 is a Cdc42 GEF inhibitor that blocks the interaction between Cdc42 and intersectin, leading to a decrease in active Cdc42. This would enhance the activity of ARHGAP11A as it would be required to inactivate any residual active Cdc42. | ||||||
GSK 269962 | 850664-21-0 | sc-363279 sc-363279A | 10 mg 50 mg | $300.00 $1000.00 | 1 | |
GSK269962A is a potent inhibitor of ROCK1 and ROCK2. By inhibiting these kinases, it leads to an increase in GTP-bound RhoA levels, thereby indirectly enhancing the activity of ARHGAP11A, which functions to catalyze the hydrolysis of GTP on RhoA. | ||||||