KLHL8 inhibitors belong to a specific class of chemical compounds that target the Kelch-like protein 8 (KLHL8), a substrate adaptor for the Cullin3 (CUL3)-dependent E3 ubiquitin ligase complex. The KLHL8 protein is involved in the regulation of various cellular processes, particularly the ubiquitination and subsequent degradation of specific protein substrates. Inhibitors of KLHL8 are designed to interfere with this ubiquitin-proteasome system, modulating the degradation of target proteins implicated in diverse cellular functions. The structural basis of KLHL8 inhibition lies in the binding of these inhibitors to the Kelch domain of the KLHL8 protein, disrupting its interaction with substrate proteins and thereby preventing their ubiquitination.
The development of KLHL8 inhibitors stems from a growing interest in understanding the intricacies of the ubiquitin-proteasome system and its role in cellular homeostasis. Researchers aim to unravel the specific substrates targeted by KLHL8 and elucidate the downstream cellular pathways affected by its inhibition. By dissecting the molecular mechanisms underlying KLHL8 inhibition, scientists seek to gain insights into the broader regulatory networks governing cellular processes such as signal transduction, protein stability, and cellular response to various stimuli.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $63.00 $158.00 $326.00 | 233 | |
Rapamycin binds to FKBP12 and the complex inhibits mTOR (mammalian target of Rapamycin), which is a part of the PI3K/AKT/mTOR pathway. Since KLHL8 is involved in cellular growth processes that mTOR regulates, inhibition of mTOR would lead to downregulation of KLHL8 function. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY294002 is a specific inhibitor of phosphoinositide 3-kinases (PI3K). PI3K inhibition leads to a downstream reduction in AKT phosphorylation and subsequent mTOR pathway activity, which indirectly can decrease KLHL8's functional activity related to cell growth and survival. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $67.00 $223.00 $425.00 | 97 | |
Wortmannin is a potent and irreversible inhibitor of PI3K. By reducing PI3K activity, wortmannin reduces AKT activation and mTOR signaling, thereby potentially inhibiting KLHL8 activity connected to these pathways. | ||||||
Triciribine | 35943-35-2 | sc-200661 sc-200661A | 1 mg 5 mg | $104.00 $141.00 | 14 | |
Triciribine specifically inhibits the phosphorylation and activation of AKT, which is downstream of PI3K. This inhibition can indirectly decrease the functional activity of KLHL8 by reducing the signaling through mTOR that is regulated by AKT. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $40.00 $92.00 | 212 | |
PD98059 is a selective inhibitor of MEK, which prevents the activation of MAPK/ERK pathway. This pathway is implicated in cell cycle progression and its inhibition could lead to a decrease in KLHL8 activity due to its role in cellular proliferation. | ||||||
U-0126 | 109511-58-2 | sc-222395 sc-222395A | 1 mg 5 mg | $64.00 $246.00 | 136 | |
U0126 is a MEK inhibitor that prevents the activation of ERK, a part of the MAPK pathway. The inhibition of this pathway can potentially reduce KLHL8 activity related to cell cycle control and proliferation. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $90.00 $349.00 | 284 | |
SB203580 is a specific inhibitor of p38 MAPK. By inhibiting p38 MAPK, it can interfere with stress response pathways and indirectly influence KLHL8 function, which may be involved in responding to cellular stress signals. | ||||||
SP600125 | 129-56-6 | sc-200635 sc-200635A | 10 mg 50 mg | $40.00 $150.00 | 257 | |
SP600125 is an inhibitor of c-Jun N-terminal kinase (JNK), which is involved in the regulation of apoptosis. Since KLHL8 can be implicated in cell survival, inhibition of JNK may indirectly affect KLHL8 functional roles in apoptosis regulation. | ||||||
Lactacystin | 133343-34-7 | sc-3575 sc-3575A | 200 µg 1 mg | $188.00 $575.00 | 60 | |
Lactacystin is a specific inhibitor of the proteasome. Since KLHL8 is known to be associated with protein ubiquitination and degradation, inhibiting the proteasome could indirectly decrease the functional activity of KLHL8 by disrupting protein turnover. | ||||||
MG-132 [Z-Leu- Leu-Leu-CHO] | 133407-82-6 | sc-201270 sc-201270A sc-201270B | 5 mg 25 mg 100 mg | $60.00 $265.00 $1000.00 | 163 | |
MG132 is a reversible proteasome inhibitor. By inhibiting the ubiquitin-proteasome pathway, MG132 could potentially lead to an accumulation of proteins that would otherwise be degraded, thus indirectly affecting KLHL8 activity in protein turnover regulation. | ||||||