LAPTM4B Inhibitors
LAPTM4B inhibitors refer to a class of chemical compounds that specifically target and modulate the activity of the lysosomal-associated transmembrane protein 4B (LAPTM4B). LAPTM4B is a transmembrane protein located primarily in lysosomal membranes, where it is implicated in regulating the intracellular trafficking of proteins and maintaining lysosomal function. It has a unique structure, consisting of four transmembrane domains, and is known to interact with various signaling pathways involved in cellular homeostasis, such as endosomal sorting and autophagy. LAPTM4B also plays a role in regulating lysosomal degradation processes, including the turnover of receptor proteins and other macromolecules. Inhibitors targeting LAPTM4B are designed to interfere with its role in these cellular mechanisms, leading to alterations in processes such as protein sorting, lysosomal stability, and intracellular signaling dynamics.
The development of LAPTM4B inhibitors typically focuses on understanding the protein's interaction with its binding partners and the structural requirements necessary for these interactions. These inhibitors are small molecules that bind to LAPTM4B, causing a disruption in its ability to participate in endosomal and lysosomal trafficking. Chemical modifications of lead compounds are often necessary to achieve high specificity for LAPTM4B over other lysosomal transmembrane proteins, ensuring that the inhibition is targeted. The chemical design of LAPTM4B inhibitors frequently incorporates molecular scaffolds that can interact with key residues in LAPTM4B's transmembrane domains or extracellular loops, disrupting its conformation or stability. As LAPTM4B is involved in fundamental cellular processes, studying its inhibitors provides insights into the regulation of lysosomal functions and their impact on intracellular signaling pathways and protein homeostasis.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Curcumin | 458-37-7 | sc-200509 sc-200509A sc-200509B sc-200509C sc-200509D sc-200509F sc-200509E | 1 g 5 g 25 g 100 g 250 g 1 kg 2.5 kg | $36.00 $68.00 $107.00 $214.00 $234.00 $862.00 $1968.00 | 47 | |
Curcumin may downregulate LAPTM4B expression by inhibiting the activation of the transcription factor NF-κB, which is presumed to play a role in the initiation of LAPTM4B gene transcription. | ||||||
Resveratrol | 501-36-0 | sc-200808 sc-200808A sc-200808B | 100 mg 500 mg 5 g | $60.00 $185.00 $365.00 | 64 | |
Resveratrol could reduce LAPTM4B expression by enhancing SIRT1 activity, leading to the deacetylation of histones associated with the LAPTM4B gene, thereby tightening chromatin structure and suppressing gene transcription. | ||||||
Quercetin | 117-39-5 | sc-206089 sc-206089A sc-206089E sc-206089C sc-206089D sc-206089B | 100 mg 500 mg 100 g 250 g 1 kg 25 g | $11.00 $17.00 $108.00 $245.00 $918.00 $49.00 | 33 | |
Quercetin is proposed to decrease LAPTM4B expression by hindering the PI3K/Akt pathway, which may be responsible for promoting the transcription of genes involved in cell survival, including LAPTM4B. | ||||||
5-Azacytidine | 320-67-2 | sc-221003 | 500 mg | $280.00 | 4 | |
5-Azacytidine may suppress LAPTM4B transcription by causing demethylation of DNA within the LAPTM4B gene promoter region, which can lead to the recruitment of transcriptional repressors and a decrease in gene expression. | ||||||
Methotrexate | 59-05-2 | sc-3507 sc-3507A | 100 mg 500 mg | $92.00 $209.00 | 33 | |
Methotrexate is known to inhibit dihydrofolate reductase, which could lead to a reduction in thymidylate synthesis, thereby hindering DNA replication and the transcriptional processes needed for LAPTM4B gene expression. | ||||||
Suberoylanilide Hydroxamic Acid | 149647-78-9 | sc-220139 sc-220139A | 100 mg 500 mg | $130.00 $270.00 | 37 | |
Suberoylanilide Hydroxamic Acid (Vorinostat) may reduce LAPTM4B expression by inhibiting histone deacetylases, which would result in a less compact chromatin structure at the LAPTM4B promoter, favoring the binding of transcriptional repressors. | ||||||
Disulfiram | 97-77-8 | sc-205654 sc-205654A | 50 g 100 g | $52.00 $87.00 | 7 | |
Disulfiram could inhibit LAPTM4B by altering the activity of the proteasome, potentially leading to the accumulation of misfolded or ubiquitinated proteins that sequester transcription factors necessary for LAPTM4B expression. | ||||||
(−)-Epigallocatechin Gallate | 989-51-5 | sc-200802 sc-200802A sc-200802B sc-200802C sc-200802D sc-200802E | 10 mg 50 mg 100 mg 500 mg 1 g 10 g | $42.00 $72.00 $124.00 $238.00 $520.00 $1234.00 | 11 | |
EGCG might inhibit LAPTM4B by suppressing the activation of NF-κB, a transcription factor that, when activated, could enhance the transcription of genes involved in cell proliferation, including LAPTM4B. | ||||||
Phenethyl isothiocyanate | 2257-09-2 | sc-205801 sc-205801A | 5 g 10 g | $102.00 $179.00 | 2 | |
Phenethyl isothiocyanate could downregulate LAPTM4B by activating the transcription factor Nrf2, which might shift cellular transcriptional mechanisms towards the expression of detoxification genes rather than LAPTM4B. | ||||||
Parthenolide | 20554-84-1 | sc-3523 sc-3523A | 50 mg 250 mg | $79.00 $300.00 | 32 | |
Parthenolide may decrease LAPTM4B expression by directly inhibiting the NF-κB pathway, which is thought to have a contributory role in promoting the transcription of the LAPTM4B gene. | ||||||