Date published: 2025-11-2

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HRT1_Hrt1 Inhibitors

Regarding the detailed description of the chemical class termed as "HRT1_Hrt1 inhibitors," which in the context of this information refers to the indirect inhibition of HEY1, these are chemicals that influence the activity of the protein by modulating the signaling pathways it is a part of, rather than directly binding to or altering the protein itself. HEY1's role as a transcriptional repressor in the Notch signaling pathway, which is implicated in diverse developmental processes and cellular functions, makes it a crucial regulatory node. Therefore, the inhibition of HEY1 typically involves the use of small molecule inhibitors that target upstream components of the Notch pathway, such as gamma-secretase, which is responsible for the release of the Notch intracellular domain, a key step in activating Notch target genes, including HEY1.

The modulation of c-Jun N-terminal kinase (JNK) activity is another strategy, given the involvement of the c-Jun pathway in the regulation of HEY1 expression. Compounds that inhibit JNK can reduce c-Jun-mediated transcription of HEY1. This indirect inhibition strategy is critical for altering the expression levels of HEY1 and its associated downstream effects on cellular processes. In addition, chemicals that affect the NF-kappaB signaling, cyclin-dependent kinases (CDKs), or the PI3K pathway may also exert an indirect inhibitory effect on HEY1 due to the interconnectedness of these pathways with Notch signaling. The breadth of this chemical class is substantial, owing to the complex and multifaceted nature of signaling pathways involved in regulating the activity of HEY1, making these chemicals pivotal in the context of biochemical research focused on transcriptional repression mechanisms.

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