DENND2C Inhibitors
DENND2C inhibitors encompass a diverse array of chemical entities that indirectly impede DENND2C activity through various cellular mechanisms. Staurosporine and Bisindolylmaleimide I, for instance, target the phosphorylation events mediated by protein kinase C, essential for DENND2C to exert its role in the activation of Rab GTPases and subsequent endocytic pathways. By curtailing PKC's function, these inhibitors effectively disrupt the upstream signaling required for DENND2C-mediated vesicle trafficking. Similarly, the ROCK inhibitor Y-27632 and Cdc42-selective inhibitor ML 141 undermine the cytoskeletal dynamics necessary for DENND2C's involvement in membrane dynamics, leading to a reduction in the protein's functional role in intracellular trafficking. LY 294002, a PI3K inhibitor, attenuates the recruitment of DENND2C to cellular membranes, consequently diminishing its catalytic activity toward Rab GTPases. Further, Wiskostatin and ZCL278, by inhibiting N-WASP and Cdc42 respectively, destabilize the actin framework required for DENND2C function, highlighting the intricate relationship between cytoskeletal organization and DENND2C's activity.
The arsenal of DENND2C inhibitors also includes compounds that disrupt various aspects of vesicular trafficking, a process to which DENND2C is intrinsically linked. Brefeldin A, for example, impedes the ARF-GTPase cycle, thereby obstructing the vesicle formation and transport processes in which DENND2C is a critical player. SecinH3 disrupts ARF-dependent trafficking by targeting cytohesins, which in turn can block the pathways upstream of DENND2C's Rab GTPase activation domain. Exo1, by hampering the exocyst complex, directly affects vesicle tethering and fusion events downstream of DENND2C's activity, thus reducing the protein's influence on these processes. Lastly, Gö 6976 and NSC 23766 interfere with the actin cytoskeleton and Rac1 GTPase signaling, respectively, both of which are crucial for the full functional expression of DENND2C in vesicular movement and cytoskeletal dynamics, further illustrating the breadth of mechanisms employed by DENND2C inhibitors to diminish the protein's activity in cellular trafficking pathways.
SEE ALSO...
Items 1 to 10 of 12 total
Display:
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Gö 6976 | 136194-77-9 | sc-221684 | 500 µg | $223.00 | 8 | |
Gö 6976 is a protein kinase C inhibitor which, by inhibiting classical PKC isoforms, may decrease the phosphorylation of substrates involved in vesicular trafficking where DENND2C functions as a GEF (guanine nucleotide exchange factor) for Rab GTPases, thereby reducing DENND2C-mediated endocytic pathway activation. | ||||||
NSC 23766 | 733767-34-5 | sc-204823 sc-204823A | 10 mg 50 mg | $148.00 $597.00 | 75 | |
NSC 23766 inhibits Rac1 by blocking its interaction with GEFs, which are crucial for actin organization. As DENND2C-mediated activation of Rab GTPases plays a role in vesicle movement that is dependent on the actin cytoskeleton, NSC 23766 can indirectly diminish the functional role of DENND2C by disrupting actin polymerization. | ||||||
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $150.00 $388.00 | 113 | |
Staurosporine is a potent nonspecific inhibitor of protein kinases. While it inhibits a broad range of kinases, its interaction with protein kinase C (PKC) can diminish PKC-mediated phosphorylation events that are upstream of DENND2C activation, leading to reduced DENND2C-mediated guanine nucleotide exchange on Rab proteins and subsequent inhibition of Rab-dependent endocytic pathways. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
Bisindolylmaleimide I is a specific inhibitor of PKC. By inhibiting PKC, it prevents the phosphorylation of proteins that are required for the activation of DENND2C. This leads to a decrease in DENND2C-mediated activation of Rab GTPases, which are involved in vesicle trafficking, and thus indirectly diminishes DENND2C function. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $182.00 $693.00 | 88 | |
Y-27632 is an inhibitor of ROCK (Rho-associated protein kinase), which is involved in actin cytoskeleton organization. Inhibition of ROCK can lead to reduced cytoskeletal rearrangements necessary for the membrane dynamics that DENND2C is involved in during the activation of Rab GTPases, decreasing DENND2C's functional role in mediating intracellular trafficking. | ||||||
ML 141 | 71203-35-5 | sc-362768 sc-362768A | 5 mg 25 mg | $134.00 $502.00 | 7 | |
ML 141 is a selective inhibitor of Cdc42 GTPase. By inhibiting Cdc42, ML 141 disrupts actin polymerization and cell motility pathways that may be required for DENND2C-mediated endocytic processes. Consequently, DENND2C's role in vesicle formation and trafficking can be diminished due to the inhibition of proper cytoskeletal organization. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY 294002 is a PI3K inhibitor which suppresses phosphoinositide 3-kinase signaling. PI3K is crucial for the initiation of many signaling cascades, including those that involve DENND2C-mediated Rab GTPase activation. By inhibiting PI3K, LY 294002 can diminish the membrane recruitment of DENND2C and therefore reduce its ability to activate Rab GTPases involved in vesicular transport processes. | ||||||
Wiskostatin | 253449-04-6 | sc-204399 sc-204399A sc-204399B sc-204399C | 1 mg 5 mg 25 mg 50 mg | $48.00 $122.00 $432.00 $812.00 | 4 | |
Wiskostatin is a specific inhibitor of the N-WASP, which is a regulator of actin polymerization. DENND2C functions are closely tied to the actin cytoskeleton dynamics; therefore, inhibition of N-WASP by Wiskostatin could reduce the cytoskeletal rearrangements essential for DENND2C's role in membrane trafficking through Rab GTPases, thus diminishing DENND2C's function. | ||||||
Brefeldin A | 20350-15-6 | sc-200861C sc-200861 sc-200861A sc-200861B | 1 mg 5 mg 25 mg 100 mg | $30.00 $52.00 $122.00 $367.00 | 25 | |
Brefeldin A disrupts the ARF-GTPase cycle, which is necessary for vesicular trafficking, a process DENND2C indirectly participates in through its interaction with Rab GTPases. By inhibiting this cycle, Brefeldin A can prevent the proper functioning of DENND2C in vesicle formation and transport. | ||||||
ZCL278 | 587841-73-4 | sc-507369 | 10 mg | $115.00 | ||
ZCL278 is a Cdc42 GTPase inhibitor which prevents the interaction of Cdc42 with its effector proteins. Since Cdc42 is implicated in pathways that DENND2C may influence through its activation of Rab GTPases, inhibiting Cdc42 can disrupt processes necessary for DENND2C function, such as actin cytoskeleton dynamics and cell motility. | ||||||