DEPTOR Inhibitors
DEPTOR, or DEP domain-containing mTOR-interacting protein, is a critical regulator of the mammalian target of rapamycin (mTOR) signaling pathway, which plays pivotal roles in various cellular processes including cell growth, proliferation, metabolism, and survival. As its name suggests, DEPTOR interacts with mTOR, a serine/threonine kinase that exists in two distinct complexes: mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2). DEPTOR functions as an endogenous inhibitor of both mTOR complexes, serving to modulate their activity and downstream signaling events. Specifically, DEPTOR binds to mTOR complexes and inhibits their kinase activity, thereby suppressing the phosphorylation of downstream targets such as ribosomal protein S6 kinase (S6K) and eukaryotic translation initiation factor 4E-binding protein 1 (4E-BP1), which are involved in protein synthesis and cell growth.
The inhibition of DEPTOR can occur through various mechanisms that disrupt its interaction with mTOR complexes or enhance its degradation, leading to dysregulated mTOR signaling and aberrant cellular functions. One such mechanism involves the activation of signaling pathways that promote the degradation of DEPTOR via the ubiquitin-proteasome system. Additionally, post-translational modifications such as phosphorylation or acetylation may modulate DEPTOR stability and activity. Furthermore, small molecules or compounds that directly bind to DEPTOR or its interacting domains can interfere with its inhibitory function, thereby unleashing mTOR activity and promoting downstream signaling cascades. Overall, the inhibition of DEPTOR represents a crucial strategy for manipulating mTOR signaling pathways and in modulating cellular processes implicated in various physiological and pathological conditions.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Torin 1 | 1222998-36-8 | sc-396760 | 10 mg | $245.00 | 7 | |
Torin 1 is a direct inhibitor of DEPTOR, functioning by inhibiting mTORC1 and mTORC2 complexes. By preventing DEPTOR inhibition of mTOR, Torin 1 modulates the PI3K-Akt pathway, suppressing cell growth and proliferation. | ||||||
AZD8055 | 1009298-09-2 | sc-364424 sc-364424A | 10 mg 50 mg | $163.00 $352.00 | 12 | |
AZD8055 is a potent DEPTOR inhibitor that targets mTOR. It specifically inhibits mTOR kinase activity, disrupting the DEPTOR-mTOR interaction. This leads to the modulation of downstream signaling pathways, hampering cellular growth and survival. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $63.00 $158.00 $326.00 | 233 | |
Rapamycin indirectly inhibits DEPTOR by binding to mTORC1. This interaction prevents DEPTOR from inhibiting mTOR, resulting in the modulation of the PI3K-Akt pathway and subsequent inhibition of cell proliferation. | ||||||
PP242 | 1092351-67-1 | sc-301606A sc-301606 | 1 mg 5 mg | $57.00 $172.00 | 8 | |
PP242 is a selective DEPTOR inhibitor that targets mTOR kinase activity. By disrupting the DEPTOR-mTOR interaction, PP242 modulates the PI3K-Akt pathway, inhibiting cell growth and survival. | ||||||
KU 0063794 | 938440-64-3 | sc-361219 | 10 mg | $209.00 | ||
Ku-0063794 inhibits DEPTOR by targeting mTOR. It disrupts the DEPTOR-mTOR interaction, leading to the inhibition of mTORC1 and mTORC2 complexes. This modulates the PI3K-Akt pathway, suppressing cellular proliferation. | ||||||
INK 128 | 1224844-38-5 | sc-364511 sc-364511A | 5 mg 50 mg | $321.00 $1835.00 | ||
INK128 is a dual mTORC1 and mTORC2 inhibitor, indirectly inhibiting DEPTOR. It disrupts the DEPTOR-mTOR interaction, modulating the PI3K-Akt pathway and inhibiting cell growth and survival. | ||||||
WYE-354 | 1062169-56-5 | sc-364652 sc-364652A | 10 mg 50 mg | $286.00 $1200.00 | ||
WYE-354 is a selective DEPTOR inhibitor that targets mTOR. By disrupting the DEPTOR-mTOR interaction, WYE-354 modulates the PI3K-Akt pathway, leading to the inhibition of cell proliferation and survival. | ||||||
OSI-027 | 936890-98-1 | sc-364557 sc-364557A | 10 mg 50 mg | $437.00 $1186.00 | 1 | |
OSI-027 is a DEPTOR inhibitor that targets mTOR. It disrupts the DEPTOR-mTOR interaction, modulating the PI3K-Akt pathway and suppressing cell growth and survival. | ||||||
N-Ethyl-N′-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea | 1207360-89-1 | sc-496573 | 5 mg | $480.00 | ||
Also called GDC-0349, this compound inhibits DEPTOR by targeting mTOR kinase activity. By disrupting the DEPTOR-mTOR interaction, GDC-0349 modulates the PI3K-Akt pathway, leading to the inhibition of cell proliferation and survival. | ||||||