RGL3 Inhibitors
Chemical inhibitors of RGL3 encompass a range of molecules that can impede the protein's function by targeting different aspects of its activity and interaction with other proteins. GTPγS, a non-hydrolyzable analog of GTP, can inhibit GTPases by binding to their active sites and preventing the release of gamma phosphate. This action directly impacts RGL3, which serves as a guanine nucleotide dissociation stimulator for Ral GTPases. By preventing the conformational changes necessary for Ral protein activation, GTPγS effectively inhibits RGL3's ability to perform its role in activating these proteins. Manumycin A, a farnesyltransferase inhibitor, blocks the farnesylation of RGL3, which is crucial for its interaction with Ral GTPases. The inhibition of this post-translational modification prevents RGL3 from associating with Ral GTPases, thereby stifling its function.
Further, Brefeldin A disrupts the Golgi apparatus by inhibiting ADP-ribosylation factor, a small GTPase involved in vesicle formation, which can indirectly affect RGL3 function due to its role in vesicle trafficking mediated by Ral GTPases. Similarly, Lovastatin impedes the biosynthesis of isoprenoids by inhibiting HMG-CoA reductase. As isoprenylation is a modification that influences RGL3 activity, Lovastatin's action can indirectly reduce the protein's ability to facilitate Ral GTPase activation. Other inhibitors like Exoenzyme C3, NSC23766, SecinH3, ML141, and ZCL278 do not target RGL3 directly but can impact its function indirectly by modulating the activity of GTPases that influence or interact with RGL3-mediated pathways. Exoenzyme C3 inactivates Rho GTPases, potentially altering signaling pathways that affect RGL3 function with Ral GTPases. NSC23766 disrupts Rac1 interactions, SecinH3 inhibits cytohesins, and ML141 and ZCL278 inhibit Cdc42, all leading to changes in cellular dynamics where RGL3 is implicated. Lastly, CID2950007 targets PIP5K, which while not directly affecting RGL3, can alter phosphatidylinositol levels and potentially modify RGL3's associated signaling cascades.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Guanosine 5′-O-(3-thiotriphosphate) tetralithium salt | 94825-44-2 | sc-202639 | 10 mg | $465.00 | ||
GTPγS is a non-hydrolyzable analog of GTP that can inhibit GTPases by preventing the release of gamma phosphate. RGL3, being a Ral guanine nucleotide dissociation stimulator, facilitates the activation of Ral GTPases. By binding to the active sites of these GTPases, GTPγS can prevent the necessary conformational changes RGL3 induces in Ral proteins, thereby inhibiting its function. | ||||||
Brefeldin A | 20350-15-6 | sc-200861C sc-200861 sc-200861A sc-200861B | 1 mg 5 mg 25 mg 100 mg | $31.00 $53.00 $124.00 $374.00 | 25 | |
Brefeldin A disrupts the Golgi apparatus structure and function by inhibiting ADP-ribosylation factor (Arf), a small GTPase involved in vesicle formation. Since RGL3 can interact with Ral GTPases, which are involved in vesicle trafficking, the disruption of Golgi function by Brefeldin A can indirectly inhibit RGL3 through the impairment of vesicular transport pathways. | ||||||
Lovastatin | 75330-75-5 | sc-200850 sc-200850A sc-200850B | 5 mg 25 mg 100 mg | $29.00 $90.00 $339.00 | 12 | |
Lovastatin inhibits HMG-CoA reductase, which is crucial for biosynthesis of cholesterol and isoprenoids. Since RGL3 activity is modulated by isoprenylation, the inhibition of isoprenoid synthesis by Lovastatin can indirectly inhibit RGL3's ability to facilitate Ral GTPase activation, as these post-translational modifications are essential for its function. | ||||||
Manumycin A | 52665-74-4 | sc-200857 sc-200857A | 1 mg 5 mg | $219.00 $634.00 | 5 | |
Manumycin A is a farnesyltransferase inhibitor that prevents the farnesylation of CAAX motif-containing proteins. RGL3, when farnesylated, can interact with Ral GTPases. Inhibition of farnesylation by Manumycin A would therefore inhibit RGL3's interaction with Ral GTPases, leading to a functional inhibition of RGL3's role in activating these proteins. | ||||||
SecinH3 | 853625-60-2 | sc-203260 | 5 mg | $278.00 | 6 | |
SecinH3 is an inhibitor of cytohesins, which are Arf-GEFs. By inhibiting cytohesins, SecinH3 can affect Arf GTPase activity. As RGL3 functionally interacts with Ral GTPases, and Arf GTPases can interact with Ral GTPases, the inhibition of Arf GTPases by SecinH3 could indirectly inhibit RGL3 function by disrupting Ral GTPase signaling pathways. | ||||||
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. Cdc42 is involved in actin polymerization and cell morphology changes. Since RGL3 is associated with Ral GTPases that can influence cellular dynamics, the inhibition of Cdc42 by ML141 can reduce the cellular actions in which RGL3 participates, thereby indirectly inhibiting RGL3. | ||||||
ZCL278 | 587841-73-4 | sc-507369 | 10 mg | $115.00 | ||
ZCL278 is a Cdc42 GTPase inhibitor that blocks the binding of Cdc42 to its effector proteins. RGL3, by modulating Ral GTPase activity, may interact with pathways involving Cdc42. The inhibition of Cdc42 by ZCL278 can therefore indirectly inhibit RGL3 by altering the cellular functions associated with Ral GTPases, such as cytoskeletal organization. | ||||||