Date published: 2025-9-22

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PXK Inhibitors

Chemical inhibitors of PXK function by interfering with various signaling pathways and enzyme activities that PXK is associated with. Staurosporine and Bisindolylmaleimide operate by targeting protein kinases that PXK is known to interact with. Staurosporine is a broad-spectrum kinase inhibitor that disrupts kinase activity essential for PXK function in signal transduction pathways. Similarly, Bisindolylmaleimide specifically inhibits Protein Kinase C (PKC), and because PXK utilizes its PX domain to interact with PKC, this interaction is essential for PXK's role in transducing signals within the cell. The PI3K inhibitors LY294002 and Wortmannin obstruct the PI3K pathway, which is crucial for PXK's involvement in cellular signaling. Inhibiting PI3K leads to a cascade effect that ultimately disrupts PXK's functionality. PP2 and Dasatinib, which inhibit Src family tyrosine kinases and a broader range of tyrosine kinases, respectively, prevent phosphorylation events that PXK requires to function within signaling pathways.

Further, U0126, SP600125, and SB203580 inhibit various components of the MAPK pathway, such as MEK, JNK, and p38 MAPK. PXK's interaction with the MAPK pathway means that disruption of these kinases can lead to reduced signaling and thus diminished PXK activity. NF449, which targets the Gs-alpha subunit of G-proteins, disrupts G-protein-coupled signaling pathways that PXK is part of, leading to an inhibition of its role in these pathways. Go6983, another PKC inhibitor, like Bisindolylmaleimide, ensures that the interaction between PXK and PKC is inhibited, which is vital for PXK's function in signal transduction. Lastly, Y-27632 inhibits ROCK kinase, which impacts the actin cytoskeleton organization. Since PXK is implicated in cytoskeletal dynamics, inhibition of ROCK kinase by Y-27632 can lead to disrupted signaling pathways that PXK is involved in, thereby inhibiting its functional role in cellular processes.

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