Date published: 2025-9-20

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TMEM81 Inhibitors

TMEM81 Inhibitors are chemically diverse entities that exert their inhibitory effects on the functional activity of TMEM81 through indirect interactions with various cellular signaling cascades and regulatory mechanisms. Inhibitors such as Wortmannin and LY 294002 target the phosphatidylinositol 3-kinase (PI3K) pathway, leading to a dampened AKT signaling cascade. This reduction in PI3K/AKT signaling can indirectly affect TMEM81's function as this pathway plays a crucial role in a multitude of cellular processes, including growth and survival, where TMEM81 could potentially be involved. Furthermore, Rapamycin, by inhibiting the mammalian target of rapamycin (mTOR) pathway, may influence the trafficking and turnover of TMEM81, which could lead to its diminished membrane stability or localization, indirectly reducing its activity.

Additional inhibitors operate through different mechanisms but result in comparable outcomes for TMEM81 function. Cyclopamine, by hindering Smoothened in the Hedgehog signaling pathway, can affect the endosomal sorting and trafficking that are essential for the proper localization and function of TMEM81. U0126 and PD 98059, both targeting the MAPK signaling pathway via MEK inhibition, and SB 203580, a p38 MAPK inhibitor, can modulate cellular stress responses and differentiation processes that indirectly involve TMEM81. By disrupting the cytoskeletal dynamics and cell motility through ROCK kinase inhibition, Y-27632 may alter the activity of TMEM81. And Bafilomycin A1, through its action on V-ATPase, could affect the endolysosomal trafficking of TMEM81. These inhibitors, by targeting various kinases and signaling molecules, contribute to a multifaceted regulatory environment where TMEM81's activity is indirectly modulated through changes in cellular signaling, trafficking, and regulatory processes.

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