HES7 Inhibitors
Chemical inhibitors of HES7 target the Notch signaling pathway, which is pivotal for the protein's functional expression. Gamma-secretase inhibitors such as DAPT, LY-411575, RO4929097, PF-03084014, MK-0752, Avagacestat, Semagacestat, Begacestat, BMS-708163, L-685,458, and Compound E all share a common mechanism of action that leads to the functional inhibition of HES7. These chemicals act by obstructing the proteolytic activity of gamma-secretase, an enzyme indispensable for the cleavage of Notch receptors. This cleavage is a prerequisite for the translocation of the Notch intracellular domain into the nucleus, where it can induce the transcription of target genes, including HES7. By preventing this cleavage, these inhibitors impair the signaling cascade necessary for HES7 activity.
The action of these inhibitors effectively reduces the transcriptional activation of HES7 by disrupting the upstream signaling events. For example, DAPT, LY-411575, and RO4929097 bind to the active site of gamma-secretase, altering its conformation and enzyme activity, which is crucial for the liberation of the Notch intracellular domain. Similarly, PF-03084014 and MK-0752 inhibit the processing of the Notch receptor, which is necessary for the initiation of the signaling cascade that leads to HES7 expression. Other inhibitors like Avagacestat, Semagacestat, and Begacestat also contribute to this mechanism, preventing the Notch pathway from performing its role in HES7 activation.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
DAPT | 208255-80-5 | sc-201315 sc-201315A sc-201315B sc-201315C | 5 mg 25 mg 100 mg 1 g | $40.00 $120.00 $480.00 $2141.00 | 47 | |
DAPT is a gamma-secretase inhibitor. HES7 is a downstream target of the Notch signaling pathway, which requires gamma-secretase for activation. Inhibition of gamma-secretase by DAPT prevents the cleavage of the Notch receptor, thus blocking the release of the Notch intracellular domain that would otherwise enter the nucleus to influence transcription of HES7. Therefore, DAPT functionally inhibits HES7 by preventing its transcriptional activation via the Notch pathway. | ||||||
LY411575 | 209984-57-6 | sc-364529 sc-364529A | 10 mg 50 mg | $198.00 $473.00 | 6 | |
LY-411575 serves as another potent gamma-secretase inhibitor. By impeding the activity of gamma-secretase, LY-411575 effectively inhibits the Notch signaling cascade, which is crucial for the activation of HES7. The disruption of Notch signaling indirectly prevents the transcription factors from initiating HES7 expression, leading to functional inhibition. | ||||||
RO-4929097 | 847925-91-1 | sc-364602 sc-364602A | 10 mg 50 mg | $439.00 $1417.00 | 1 | |
RO4929097 is a gamma-secretase inhibitor that disrupts the Notch signaling pathway. By blocking gamma-secretase, RO4929097 inhibits the cleavage of Notch receptors and the subsequent signaling required for HES7 activity, thereby leading to functional inhibition of HES7 expression. | ||||||
PF-3084014 | 1290543-63-3 | sc-507501 | 5 mg | $130.00 | ||
PF-03084014, also a gamma-secretase inhibitor, suppresses Notch receptor processing and impairs the signaling necessary for HES7 function. With the Notch pathway inhibited, the initiation and maintenance of HES7 activity are disrupted, resulting in functional inhibition of the protein. | ||||||
MK-0752 | 471905-41-6 | sc-364534 sc-364534A | 10 mg 50 mg | $592.00 $1550.00 | ||
MK-0752 is a gamma-secretase inhibitor that interferes with the proteolytic cleavage of Notch receptors. This interruption of Notch signaling halts the downstream gene activation, including that of HES7, thereby functionally inhibiting the protein. | ||||||
BMS-708163 | 1146699-66-2 | sc-364444 sc-364444A | 10 mg 50 mg | $480.00 $1455.00 | 1 | |
Avagacestat is a gamma-secretase inhibitor that, by blocking the cleavage of Notch receptors, disrupts the Notch signaling pathway needed for the transcriptional activation of HES7, leading to its functional inhibition. | ||||||
Semagacestat | 425386-60-3 | sc-364614 sc-364614A | 10 mg 50 mg | $350.00 $1200.00 | 1 | |
As a gamma-secretase inhibitor, Semagacestat prevents the activation of Notch signaling pathway components, thus inhibiting the signaling cascade that normally results in HES7 expression and function. | ||||||
L-685,458 | 292632-98-5 | sc-204042 sc-204042A | 1 mg 5 mg | $337.00 $1000.00 | 4 | |
L-685,458 is an inhibitor of gamma-secretase, an enzyme required for Notch signaling activation. By inhibiting this enzyme, L-685,458 indirectly prevents the activation of HES7, resulting in its functional inhibition. | ||||||
Compound E | 209986-17-4 | sc-221433 sc-221433A sc-221433B | 250 µg 1 mg 5 mg | $124.00 $342.00 $967.00 | 12 | |
Compound E is a potent and selective gamma-secretase inhibitor. It disrupts the Notch signaling pathway by inhibiting the cleavage of Notch receptors, which is a crucial step for the activation of HES7, thus functionally inhibiting the protein. | ||||||