Date published: 2025-9-12

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BKS Inhibitors

Chemical inhibitors of BKS can disrupt its signaling functions through a variety of molecular mechanisms. Wortmannin and LY294002, for instance, target phosphoinositide 3-kinases (PI3Ks), key enzymes in the PI3K/Akt signaling pathway which is often crucial for protein functions related to cell survival, proliferation, and metabolism. By inhibiting PI3K, these chemicals prevent the phosphorylation of phosphatidylinositol 4,5-bisphosphate (PIP2) to phosphatidylinositol 3,4,5-trisphosphate (PIP3). This inhibition can impede the activation of downstream targets that BKS may act upon or with, thereby impeding BKS's functionality in cellular signaling. Similarly, specific kinase inhibitors such as Dasatinib and PP2 interfere with Src family kinases. Since Src kinases are involved in various signaling pathways, their inhibition by these chemicals can disrupt the functional activity of BKS if it is associated with Src-mediated signaling pathways.

Further inhibitory effects on BKS come from chemicals like U0126, PD98059, SB203580, and SP600125, which target different mitogen-activated protein kinases (MAPKs). U0126 and PD98059 specifically inhibit MEK1/2, thereby blocking the activation of extracellular signal-regulated kinases (ERKs), which could be necessary for BKS's role in certain signaling pathways. SB203580, on the other hand, inhibits p38 MAPK, and SP600125 inhibits c-Jun N-terminal kinase (JNK), both of which are part of the MAPK family. These inhibitors can disrupt the MAPK signaling cascade, leading to a decrease in BKS's activity if it is regulated by MAPK. Additionally, GF109203X and Go6983, as inhibitors of protein kinase C (PKC), can impede signaling pathways where BKS's functionality is contingent upon PKC-mediated phosphorylation. Finally, mTOR inhibitors like Rapamycin and AZD8055 can have a substantial effect on BKS by blocking the mTOR pathway, which is critical for cell growth and proliferation. AZD8055 specifically targets both mTORC1 and mTORC2 complexes, which could be essential for BKS's activity in related signaling networks. Each of these chemicals, by targeting specific kinases or signaling pathways, can significantly alter the functional landscape in which BKS operates within the cell.

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