Date published: 2026-4-1

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ARHGEF5_Arhgef5 Inhibitors

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.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Y-27632, free base

146986-50-7sc-3536
sc-3536A
5 mg
50 mg
$186.00
$707.00
88
(1)

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

733767-34-5sc-204823
sc-204823A
10 mg
50 mg
$151.00
$609.00
75
(4)

An inhibitor of Rac1 GTPase, one of the targets of ARHGEF5. NSC 23766 prevents the activation of Rac1, thereby inhibiting ARHGEF5.

EHT 1864

754240-09-0sc-361175
sc-361175A
10 mg
50 mg
$213.00
$889.00
12
(2)

A Rac GTPase inhibitor. By preventing Rac activation, EHT 1864 can indirectly inhibit ARHGEF5.

ML 141

71203-35-5sc-362768
sc-362768A
5 mg
25 mg
$137.00
$512.00
7
(1)

A selective inhibitor of Cdc42 GTPase, which influences Rho GTPase activity. Inhibiting Cdc42 with ML141 can indirectly disrupt ARHGEF5.

ITX 3

347323-96-0sc-295214
sc-295214A
10 mg
50 mg
$145.00
$615.00
(0)

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

1173671-63-0sc-507401
25 mg
$555.00
(0)

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

587841-73-4sc-507369
10 mg
$115.00
(0)

A selective inhibitor of Cdc42 GTPase. By inhibiting Cdc42, which influences the activity of Rho GTPases, ZCL278 can indirectly disrupt ARHGEF5.

SecinH3

853625-60-2sc-203260
5 mg
$278.00
6
(1)

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

425399-05-9sc-397016
10 mg
$460.00
1
(0)

An inhibitor of Cdc42 GTPase. By inhibiting Cdc42, which influences Rho GTPase activity, CASIN can indirectly disrupt ARHGEF5.

Tozasertib

639089-54-6sc-358750
sc-358750A
25 mg
50 mg
$62.00
$87.00
4
(1)

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.