HSF3 Inhibitors
Chemical inhibitors of Heat Shock Transcription Factor 3 (HSF3) operate through various mechanisms to impede its function. Quercetin achieves this by stabilizing HSF3 in an inactive state, thereby hindering its capacity to trimerize and bind to DNA. Triptolide takes a similar route, obstructing the transcriptional activity of heat shock proteins by preventing HSF3 from binding to the heat shock element sequences within the DNA. This disruption directly impacts the gene expression facilitated by HSF3. KNK437 contributes to this inhibitory profile by obstructing the heat shock response, effectively preventing the activation and nuclear translocation of HSF3 which is critical for the induction of heat shock proteins. Myricetin and Quercitrin, on the other hand, interact with HSF3 to impede its DNA-binding activity.
Furthermore, Celastrol's inhibition mechanism involves the induction of high-molecular-weight complexes of a closely related heat shock factor, suggesting that it would similarly affect HSF3, resulting in a transcriptionally inactive state. Emunin limits HSF3 by altering post-translational modifications essential for the activation of this transcription factor. Epigallocatechin gallate (EGCG) joins this group by binding to HSF3 and preventing the critical steps of activation and nuclear translocation. Paeonol and Tanshinone IIA also contribute to the inhibition of HSF3 by interfering with its activation process, including the crucial phosphorylation step for Paeonol and impacting the DNA-binding activity for Tanshinone IIA. Each of these chemicals, through their distinct interactions with HSF3, play a role in inhibiting the regulatory function it plays in the expression of heat shock proteins.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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 $110.00 $250.00 $936.00 $50.00 | 33 | |
Quercetin inhibits the heat shock transcription factor 3 (HSF3) by stabilizing HSF3 in its inactive form. Quercetin has been shown to bind to the regulatory domain of HSF and prevent its trimerization, which is necessary for DNA binding. | ||||||
Triptolide | 38748-32-2 | sc-200122 sc-200122A | 1 mg 5 mg | $90.00 $204.00 | 13 | |
Triptolide inhibits HSF3 by preventing the transcriptional activity of heat shock proteins. It has been observed to inhibit the binding of HSF to heat shock element (HSE) sequences in DNA, thereby inhibiting HSF3-mediated gene expression. | ||||||
Heat Shock Protein Inhibitor I | 218924-25-5 | sc-221709 | 5 mg | $97.00 | 5 | |
KNK437 acts as an inhibitor of HSF3 by blocking the heat shock response. It inhibits the induction of heat shock proteins, likely by interacting with HSF and preventing its activation and nuclear translocation. | ||||||
KRIBB11 | 342639-96-7 | sc-507391 | 5 mg | $95.00 | ||
KRIBB11 directly inhibits the transcriptional activity of HSF1, and by extension, it can be hypothesized to inhibit HSF3, as it prevents the formation of the active DNA-binding form of HSF. | ||||||
Myricetin | 529-44-2 | sc-203147 sc-203147A sc-203147B sc-203147C sc-203147D | 25 mg 100 mg 1 g 25 g 100 g | $97.00 $188.00 $260.00 $510.00 $1022.00 | 3 | |
Myricetin inhibits HSF3 by directly interacting with the heat shock factor and preventing its DNA-binding activity, thus inhibiting the transcriptional activity of heat shock proteins that HSF3 regulates. | ||||||
Celastrol, Celastrus scandens | 34157-83-0 | sc-202534 | 10 mg | $158.00 | 6 | |
Celastrol inhibits HSF3 by inducing the formation of high-molecular-weight HSF1 complexes, which are transcriptionally inactive. It is assumed that celastrol would similarly affect HSF3, inhibiting its functional activity. | ||||||
(−)-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 | $43.00 $73.00 $126.00 $243.00 $530.00 $1259.00 | 11 | |
Epigallocatechin gallate inhibits HSF3 by binding to HSF and preventing its activation and nuclear translocation, which are necessary steps for HSF3 to initiate transcription of heat shock proteins. | ||||||
Paeonol | 552-41-0 | sc-205787 sc-205787A | 1 g 5 g | $34.00 $163.00 | 1 | |
Paeonol inhibits HSF3 by interfering with the heat shock response, potentially by blocking HSF phosphorylation which is a key regulatory step in HSF activation and function. | ||||||
Tanshinone IIA | 568-72-9 | sc-200932 sc-200932A | 5 mg 25 mg | $88.00 $316.00 | 22 | |
Tanshinone IIA inhibits HSF3 by affecting its activation and DNA-binding activity. It is known to inhibit the activity of other transcription factors and could similarly impact HSF3's ability to promote heat shock protein expression. | ||||||