The protein ARHGEF5_Arhgef5, also known as Rho guanine nucleotide exchange factor 5, is a key regulator of Rho GTPases, crucial mediators of cytoskeletal dynamics, cell migration, and cellular adhesion. ARHGEF5_Arhgef5 acts as a guanine nucleotide exchange factor (GEF), facilitating the activation of Rho GTPases by catalyzing the exchange of GDP for GTP, thereby promoting their active state. Through its GEF activity, ARHGEF5_Arhgef5 regulates various cellular processes, including actin cytoskeleton organization, cell polarity, and cell motility, essential for tissue morphogenesis and homeostasis. Additionally, ARHGEF5_Arhgef5 has been implicated in diverse signaling pathways and cellular functions, including cell proliferation, survival, and differentiation, further underscoring its significance in cellular physiology and development.
Inhibition of ARHGEF5_Arhgef5 activity represents a viable strategy for modulating cellular processes associated with its function. Several mechanisms have been proposed for inhibiting ARHGEF5_Arhgef5, including small molecule inhibitors targeting its catalytic domain or allosteric sites. Additionally, RNA interference-based approaches aimed at silencing ARHGEF5_Arhgef5 expression have shown promise in attenuating its activity. Moreover, competitive inhibitors that disrupt protein-protein interactions involving ARHGEF5_Arhgef5 and its binding partners have demonstrated efficacy in studies. Elucidating the precise structural and functional characteristics of ARHGEF5_Arhgef5 and its regulatory mechanisms is essential for the rational design of effective inhibitors. Overall, understanding the mechanisms of ARHGEF5_Arhgef5 inhibition holds promise for uncovering novel avenues for diseases associated with its dysregulation.
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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 | $186.00 $707.00 | 88 | |
A selective inhibitor of ROCK (Rho-associated coiled-coil kinase), a downstream effector of Rho GTPases including RhoA. By inhibiting ROCK, Y-27632 can disrupt the RhoA signaling pathway, consequently inhibiting ARHGEF5. | ||||||
NSC 23766 | 733767-34-5 | sc-204823 sc-204823A | 10 mg 50 mg | $151.00 $609.00 | 75 | |
An inhibitor of Rac1 GTPase, one of the targets of ARHGEF5. NSC 23766 prevents the activation of Rac1, thereby inhibiting ARHGEF5. | ||||||
EHT 1864 | 754240-09-0 | sc-361175 sc-361175A | 10 mg 50 mg | $213.00 $889.00 | 12 | |
A Rac GTPase inhibitor. By preventing Rac activation, EHT 1864 can indirectly inhibit ARHGEF5. | ||||||
ML 141 | 71203-35-5 | sc-362768 sc-362768A | 5 mg 25 mg | $137.00 $512.00 | 7 | |
A selective inhibitor of Cdc42 GTPase, which influences Rho GTPase activity. Inhibiting Cdc42 with ML141 can indirectly disrupt ARHGEF5. | ||||||
ITX 3 | 347323-96-0 | sc-295214 sc-295214A | 10 mg 50 mg | $145.00 $615.00 | ||
A selective inhibitor of Trio, which is a GEF like ARHGEF5 and shares some common targets. ITX3 can indirectly inhibit ARHGEF5 via disruption of shared signaling pathways. | ||||||
Rhosin | 1173671-63-0 | sc-507401 | 25 mg | $555.00 | ||
A selective inhibitor of RhoA GTPase, one of the targets of ARHGEF5. By inhibiting RhoA, Rhosin can disrupt the RhoA signaling pathway, thereby inhibiting ARHGEF5. | ||||||
ZCL278 | 587841-73-4 | sc-507369 | 10 mg | $115.00 | ||
A selective inhibitor of Cdc42 GTPase. By inhibiting Cdc42, which influences the activity of Rho GTPases, ZCL278 can indirectly disrupt ARHGEF5. | ||||||
SecinH3 | 853625-60-2 | sc-203260 | 5 mg | $278.00 | 6 | |
An inhibitor of cytohesins, which are GEFs like ARHGEF5 and share some common targets. SecinH3 can indirectly inhibit ARHGEF5 via disruption of shared signaling pathways. | ||||||
CASIN | 425399-05-9 | sc-397016 | 10 mg | $460.00 | 1 | |
An inhibitor of Cdc42 GTPase. By inhibiting Cdc42, which influences Rho GTPase activity, CASIN can indirectly disrupt ARHGEF5. | ||||||
Tozasertib | 639089-54-6 | sc-358750 sc-358750A | 25 mg 50 mg | $62.00 $87.00 | 4 | |
An inhibitor of Aurora kinases, which are involved in cell cycle regulation, a process in which Rho GTPases (and therefore ARHGEF5) play a role. By inhibiting Aurora kinases, Tozasertib can indirectly inhibit ARHGEF5. | ||||||