Rho H Inhibitors
Chemical inhibitors of Rho H can exert their inhibitory effects through various mechanisms, impacting the protein's activity within the cell. NSC 23766, for instance, specifically targets the interaction between Rho GTPase and its guanine nucleotide exchange factors (GEFs), which are crucial for the activation of Rho H. By preventing this interaction, NSC 23766 ensures that Rho H remains in an inactive GDP-bound state, leading to a decrease in its downstream signaling activities. Similarly, Rhosin binds directly to the guanine nucleotide binding pocket of Rho H, impeding the action of GEFs. As a result, Rhosin maintains Rho H in an inactive state and interrupts its influence on cellular processes. EHT 1864 also binds to Rho H, stabilizing it in an inactive state, which prevents Rho H from interacting with downstream effectors and thus inhibits its function.
Another layer of regulation involves the inhibition of downstream targets or related family members of Rho GTPases. For example, Y-27632 is a selective inhibitor of Rho-associated protein kinase (ROCK), a downstream effector of Rho H. By inhibiting ROCK, Y-27632 can indirectly lead to the functional inhibition of Rho H by halting the phosphorylation of downstream targets essential for Rho H-mediated signaling. CCG-1423 undermines the Rho H pathway by inhibiting the transcriptional activity of serum response factor (SRF), which is activated by Rho H signaling. This disruption in SRF activity leads to a decrease in the transcription of genes essential for Rho H functions. Moreover, ML141 and CASIN, which are specific inhibitors of Cdc42, another member of the Rho GTPase family, can influence the Rho H pathway by attenuating the cross-talk and compensatory mechanisms within the Rho GTPase family, leading to a functional inhibition of Rho H. ITX3 and CID-1067700 function by inhibiting GEFs like Trio, which activates Rho H, thus preventing the activation and subsequent signaling of Rho H.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
NSC 23766 | 733767-34-5 | sc-204823 sc-204823A | 10 mg 50 mg | $148.00 $597.00 | 75 | |
NSC 23766 specifically inhibits the interaction between Rho GTPase and its specific guanine nucleotide exchange factors (GEFs), which are essential for Rho H activation. By preventing this interaction, NSC 23766 inhibits Rho H activation, leading to a functional inhibition of its downstream signaling. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $182.00 $693.00 | 88 | |
Y-27632 is a well-characterized inhibitor of ROCK (Rho-associated protein kinase), which is downstream of Rho H signaling. By inhibiting ROCK, this compound can prevent the phosphorylation and activation of downstream targets that are critical for Rho H-mediated cellular functions, leading to functional inhibition of Rho H. | ||||||
CCG-1423 | 285986-88-1 | sc-205241 sc-205241A | 1 mg 5 mg | $30.00 $90.00 | 8 | |
CCG-1423 inhibits the transcriptional activity of serum response factor (SRF), a downstream target of Rho H signaling. By inhibiting SRF, CCG-1423 disrupts the transcription of genes that are necessary for Rho H-mediated cellular processes, thus functionally inhibiting Rho H. | ||||||
Rhosin | 1173671-63-0 | sc-507401 | 25 mg | $555.00 | ||
Rhosin directly inhibits Rho H by binding to the guanine nucleotide binding pocket, preventing the activation of Rho H by GEFs. This blockade results in the functional inhibition of Rho H's activity in the cell. | ||||||
ML 141 | 71203-35-5 | sc-362768 sc-362768A | 5 mg 25 mg | $134.00 $502.00 | 7 | |
ML141 is a specific inhibitor of Cdc42, a Rho GTPase family member. By inhibiting Cdc42, ML141 can attenuate the cross-talk within the Rho GTPase family members, potentially leading to the functional inhibition of Rho H signaling pathways. | ||||||
ITX 3 | 347323-96-0 | sc-295214 sc-295214A | 10 mg 50 mg | $145.00 $615.00 | ||
ITX3 is an inhibitor of Trio, a GEF that activates several Rho GTPases including Rho H. By inhibiting Trio, ITX3 can prevent the activation of Rho H, leading to functional inhibition of its signaling. | ||||||
EHT 1864 | 754240-09-0 | sc-361175 sc-361175A | 10 mg 50 mg | $209.00 $872.00 | 12 | |
EHT 1864 is a small molecule that binds to Rho H and inhibits its activation. By stabilizing Rho H in an inactive state, EHT 1864 prevents its interaction with downstream effectors, resulting in functional inhibition. | ||||||
2-(Benzoylcarbamothioylamino)-5,5-dimethyl-4,7-dihydrothieno[2,3-c]pyran-3-carboxylic Acid | 314042-01-8 | sc-503400 | 10 mg | $300.00 | ||
CID-1067700 competitively inhibits GEFs, which are necessary for the activation of Rho GTPases like Rho H. This compound thus prevents the exchange of GDP for GTP on Rho H, maintaining it in an inactive state and functionally inhibiting its activity. | ||||||
ZCL278 | 587841-73-4 | sc-507369 | 10 mg | $115.00 | ||
ZCL278 disrupts the interaction between Cdc42 and its GEFs, which can indirectly lead to the functional inhibition of Rho H by altering the balance and function of related Rho GTPases within the cell. | ||||||
CASIN | 425399-05-9 | sc-397016 | 10 mg | $460.00 | 1 | |
CASIN inhibits Cdc42 activity, which can lead to functional inhibition of Rho H by impacting the overall Rho GTPase signaling dynamics and downstream signaling pathways that Rho H participates in. | ||||||