Date published: 2025-10-27

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FAM54A Inhibitors

Chemical inhibitors of FAM54A can exert their inhibitory effects through interference with upstream signaling pathways essential for its function. PD 98059, U0126, and SB203580 serve as inhibitors of the MAPK pathway, with PD 98059 and U0126 specifically targeting MEK1/2 while SB203580 focuses on p38 MAP kinase. Inhibition of these kinases leads to reduced ERK and p38 MAPK activity, respectively, which are essential for the proper functioning of FAM54A. As ERK is a known mediator in the signaling pathways that FAM54A is involved in, the disruption of ERK phosphorylation by these inhibitors can result in a decrease in FAM54A activity. Similarly, by impeding the p38 MAPK, SB203580 can attenuate the stress response signals that might contribute to the regulation of FAM54A, thereby diminishing its functional capacity. Further targeting the PI3K/AKT/mTOR signaling axis, LY294002 and Wortmannin directly inhibit PI3K, while Rapamycin inhibits mTOR, a downstream target in this pathway. The inhibition of PI3K by LY294002 and Wortmannin results in reduced AKT phosphorylation and activity, which is necessary for the full activation of FAM54A. Rapamycin's inhibition of mTOR, a pivotal kinase in this pathway, similarly disrupts signals that regulate FAM54A's function. Additional inhibitors like Dasatinib and PP2 challenge the protein by inhibiting various tyrosine kinases that might phosphorylate substrates involved in the proper functioning of FAM54A, leading to an overall inhibition of its activity. AG490 targets JAK2 kinase, which, by extension, can hamper pathways that modulate FAM54A activity. SP600125, which inhibits JNK, could also suppress FAM54A function by interfering with JNK-dependent signaling mechanisms. PD173074 obstructs FGFR kinase activity, potentially leading to a reduced function of FAM54A due to the inhibition of growth factor-related pathways. Lastly, Staurosporine, as a broad-spectrum protein kinase inhibitor, can inhibit a range of kinases that may be involved in signaling pathways necessary for FAM54A activity, resulting in a comprehensive inhibition of its functional state.

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