ARHGEF17 Inhibitors
ARHGEF17 inhibitors are a group of compounds that interfere with the function of the ARHGEF17 protein, a guanine nucleotide exchange factor (GEF) that plays a pivotal role in the activation of Rho family GTPases, including RhoA, Rac1, and Cdc42. These GTPases are crucial for the regulation of the actin cytoskeleton, cell polarity, and migration. The inhibitors work through different mechanisms to reduce the functional activity of ARHGEF17, either by directly binding to it or by affecting its downstream signaling partners.
Y-27632, for instance, is a potent inhibitor of ROCK, which is a kinase that phosphorylates and activates ARHGEF17. By inhibiting ROCK, Y-27632 indirectly reduces ARHGEF17's ability to facilitate the exchange of GDP for GTP on RhoA, diminishing RhoA-mediated cellular responses. Similarly, Rhosin directly binds to RhoA and prevents its interaction with ARHGEF17, thereby effectively inhibiting the GEF activity of ARHGEF17. By blocking the ability of ARHGEF17 to activate RhoA, Rhosin indirectly leads to a decrease in RhoA-mediated signaling pathways that are essential for various cellular processes, such as cell shape maintenance and cell motility. Another example is NSC23766, which specifically inhibits the interaction between Rac1 and its GEFs, including ARHGEF17. This inhibition leads to a decrease in Rac1 activation and, consequently, a reduction in Rac1-dependent cellular functions that ARHGEF17 would typically facilitate.
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 | |
A selective inhibitor of ROCK (Rho-associated protein kinase), which phosphorylates and activates ARHGEF17, a Rho guanine nucleotide exchange factor (GEF). By inhibiting ROCK, Y-27632 indirectly inhibits ARHGEF17's activation, as ROCK-mediated phosphorylation is critical for ARHGEF17's GEF activity towards RhoA. | ||||||
Rhosin | 1173671-63-0 | sc-507401 | 25 mg | $555.00 | ||
Specifically binds to RhoA and prevents its interaction with GEFs including ARHGEF17, thereby inhibiting ARHGEF17-induced RhoA activation. This compound ensures that ARHGEF17 cannot exert its exchange factor activity on RhoA, leading to decreased RhoA-mediated signaling events. | ||||||
EHop-016 | 1380432-32-5 | sc-497382 | 5 mg | $80.00 | ||
A Rac1 inhibitor that indirectly affects ARHGEF17 by inhibiting Vav2, another GEF, which competes with ARHGEF17 for Rac1 binding. Reduced Vav2 activity can lead to increased availability of Rac1 for inhibition by other molecules, affecting the functional activity of ARHGEF17. | ||||||
ITX 3 | 347323-96-0 | sc-295214 sc-295214A | 10 mg 50 mg | $145.00 $615.00 | ||
A selective inhibitor of Trio, a GEF for Rac1 and RhoG, which can also indirectly inhibit ARHGEF17 activity by reducing overall Rac1 activation. This reduction in Rac1 activation can dampen the signaling pathways that ARHGEF17 is involved in. | ||||||
ZCL278 | 587841-73-4 | sc-507369 | 10 mg | $115.00 | ||
A small molecule that inhibits Cdc42 interaction with its GEFs, including ARHGEF17. By blocking Cdc42 activation, ARHGEF17's influence on actin cytoskeleton organization and cell morphology through Cdc42 is diminished. | ||||||
CASIN | 425399-05-9 | sc-397016 | 10 mg | $460.00 | 1 | |
Cdc42 activity-specific inhibitor that by reducing active Cdc42 levels, indirectly affects ARHGEF17's ability to promote signaling pathways that rely on Cdc42's active state. | ||||||
ML 141 | 71203-35-5 | sc-362768 sc-362768A | 5 mg 25 mg | $137.00 $512.00 | 7 | |
A selective and non-competitive inhibitor of Cdc42 that can indirectly reduce the functional activity of ARHGEF17 by decreasing the pool of active Cdc42 GTPase, which is necessary for downstream signaling. | ||||||