R9AP Inhibitors
Chemical inhibitors of R9AP operate through diverse mechanisms to impede its function within cellular signaling pathways. Palmitoyl-DL-carnitine can disrupt the lipid rafts within cellular membranes, which are essential for the localization and function of R9AP. By altering the membrane microdomains, Palmitoyl-DL-carnitine interferes with the ability of R9AP to integrate into signaling complexes effectively. Similarly, Phosphatidylinositol impacts R9AP activity by modifying the phosphoinositide composition of the membrane, crucial for R9AP's anchoring and function. This alteration in lipid signaling is another avenue through which the activity of R9AP is inhibited.
Protein kinase C (PKC) inhibitors such as Chelerythrine, Go6976, and Bisindolylmaleimide I target the phosphorylation process that is vital for R9AP's role in signal transduction. Chelerythrine, with its broad inhibitory action on PKC, and Go6976, with a more selective inhibition profile focusing on PKC alpha and beta isoforms, prevent the phosphorylation of proteins that regulate R9AP's activity. Bisindolylmaleimide I shares a similar inhibitory effect on PKC, thereby affecting R9AP indirectly. Other kinase inhibitors like PD98059 and LY294002 obstruct upstream signaling pathways that eventually lead to R9AP activity modulation. PD98059 inhibits MEK, which is upstream of ERK signaling, while LY294002 targets PI3K, thereby disrupting PI3K/Akt signaling pathways, both of which are essential for the phosphorylation and activation of proteins associated with R9AP. Genistein and PP2, as tyrosine kinase inhibitors, impede the tyrosine phosphorylation critical for the functional activity of proteins in R9AP-associated pathways. In contrast, U73122, as a PLC inhibitor, affects the PLC-dependent signaling cascade, which is an integral part of R9AP's role in G-protein coupled receptor signaling. Wiskostatin and ML7 target cytoskeletal regulators, N-WASP and MLCK respectively, impacting the cytoskeletal dynamics and associations that are crucial for the proper localization and function of R9AP within the cell.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Chelerythrine | 34316-15-9 | sc-507380 | 100 mg | $540.00 | ||
Chelerythrine is a potent inhibitor of protein kinase C (PKC), and since PKC is involved in the phosphorylation of proteins that regulate signal transduction pathways including those associated with R9AP, its inhibition can disrupt the functional activity of R9AP. | ||||||
Gö 6976 | 136194-77-9 | sc-221684 | 500 µg | $223.00 | 8 | |
Go6976 is a selective inhibitor of PKC, particularly PKC alpha and beta isoforms. By inhibiting PKC, Go6976 can hinder the phosphorylation and activity of R9AP as PKC is involved in the regulation of proteins that interact with and modulate R9AP's activity. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
Bisindolylmaleimide I is another PKC inhibitor that can prevent PKC-mediated phosphorylation, thereby potentially inhibiting R9AP activity indirectly by affecting the phosphorylation status of proteins within the R9AP-associated signaling pathways. | ||||||
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 an inhibitor of the N-WASP, a regulator of actin polymerization. Since R9AP is associated with cytoskeletal elements, inhibition of N-WASP may impede the correct localization and function of R9AP in relation to the cytoskeleton. | ||||||
ML-7 hydrochloride | 110448-33-4 | sc-200557 sc-200557A | 10 mg 50 mg | $89.00 $262.00 | 13 | |
ML7 is an inhibitor of myosin light chain kinase (MLCK). Inhibition of MLCK affects the actin cytoskeleton dynamics, which can indirectly inhibit R9AP by altering its cytoskeletal associations, potentially impeding its interaction with other signaling molecules. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $39.00 $90.00 | 212 | |
PD98059 is an inhibitor of MEK, which in turn inhibits ERK signaling. As R9AP is involved in signal transduction, hindering upstream ERK signaling could result in a decrease in R9AP function due to the lack of required phosphorylation events that are essential for its activity. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY294002 is a PI3K inhibitor, which can inhibit R9AP by interfering with PI3K/Akt signaling pathways, affecting the phosphorylation and activity of proteins that interact with R9AP, thus impeding its function. | ||||||
Genistein | 446-72-0 | sc-3515 sc-3515A sc-3515B sc-3515C sc-3515D sc-3515E sc-3515F | 100 mg 500 mg 1 g 5 g 10 g 25 g 100 g | $26.00 $92.00 $120.00 $310.00 $500.00 $908.00 $1821.00 | 46 | |
Genistein is a tyrosine kinase inhibitor, which could inhibit R9AP by interfering with tyrosine phosphorylation events that are crucial for the function of proteins within the R9AP-associated signaling pathways. | ||||||
PP 2 | 172889-27-9 | sc-202769 sc-202769A | 1 mg 5 mg | $92.00 $223.00 | 30 | |
PP2 is an inhibitor of Src family tyrosine kinases. Src kinases participate in multiple signaling pathways that could involve R9AP. Inhibition of Src kinases could therefore disrupt signal transduction processes important for R9AP function. | ||||||