HSF4 Activators
HSF4 Activators are an intriguing class of chemical compounds that play a pivotal role in modulating the cellular stress response machinery, particularly by inducing the activity of Heat Shock Factor Protein 4 (HSF4). This group of molecules encompasses a diverse array of structures and functionalities, yet they converge on a singular biological endpoint: the activation of HSF4. HSF4 is a transcriptional regulator that orchestrates the expression of heat shock proteins (HSPs), which are crucial for protein folding, repair, and degradation processes. The activation of HSF4 is primarily associated with the cellular response to various forms of proteotoxic stress, which can be triggered by an accumulation of misfolded or damaged proteins within the cell. The compounds that stimulate HSF4 do so through different mechanisms, many of which involve the perturbation of cellular homeostasis, thereby necessitating the activation of protective stress response pathways.
For instance, HSF4 activators such as geldanamycin and its derivative, 17-AAG, act by inhibiting the function of Heat Shock Protein 90 (Hsp90), a molecular chaperone that is essential for the proper folding and stabilization of many client proteins. The inhibition of Hsp90 by these compounds results in a buildup of unfolded or misfolded proteins, thereby triggering a cellular stress response that culminates in the activation of HSF4. Similarly, proteasome inhibitors like MG132 and bortezomib lead to an accumulation of polyubiquitinated proteins by blocking the degradation pathway of these proteins.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Geldanamycin | 30562-34-6 | sc-200617B sc-200617C sc-200617 sc-200617A | 100 µg 500 µg 1 mg 5 mg | $39.00 $59.00 $104.00 $206.00 | 8 | |
Geldanamycin binds to heat shock protein 90 (Hsp90) and inhibits its chaperone activity. Since Hsp90 is essential for the maturation of many signaling proteins, its inhibition by geldanamycin can lead to the activation of Heat shock factor protein 4 (HSF4) as a stress response to cope with increased levels of misfolded proteins. | ||||||
Triptolide | 38748-32-2 | sc-200122 sc-200122A | 1 mg 5 mg | $90.00 $204.00 | 13 | |
Triptolide is a diterpene triepoxide that can induce heat shock response. Through its multifaceted effects on cellular processes, it can cause protein misfolding and thus indirectly enhance the activation of HSF4 as the cell attempts to mitigate the damage. | ||||||
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 proteasome inhibitor that leads to the accumulation of polyubiquitinated proteins, inducing proteotoxic stress. This upregulates the demand for molecular chaperones and consequently activates HSF4 to enhance the cell's capacity to alleviate the stress. | ||||||
Zerumbone | 471-05-6 | sc-364148 sc-364148A | 10 mg 50 mg | $112.00 $408.00 | ||
Zerumbone is a sesquiterpene compound that can activate HSF4 indirectly by inducing cellular stress, which requires the upregulation of molecular chaperones to maintain protein homeostasis. | ||||||
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 is a flavonoid that has been shown to activate the heat shock response by modulating the expression of heat shock proteins, suggesting a potential indirect activation role for HSF4 by increasing the cellular need for chaperone 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 | |
EGCG is a catechin found in green tea that is known to induce the expression of heat shock proteins, potentially leading to the activation of HSF4, which would be required to manage the increased demand for chaperone activity. | ||||||
Quinomycin A | 512-64-1 | sc-202306 | 1 mg | $166.00 | 4 | |
Quinomycin A is a quinoxaline antibiotic that can bind to DNA and inhibit hypoxia-inducible factor 1 (HIF-1). The inhibition of HIF-1 can lead to cellular stress, potentially activating HSF4 as a compensatory mechanism to deal with the stress and restore homeostasis. | ||||||
Tunicamycin | 11089-65-9 | sc-3506A sc-3506 | 5 mg 10 mg | $172.00 $305.00 | 66 | |
Tunicamycin is an N-glycosylation inhibitor, inducing ER stress and the unfolded protein response (UPR). The UPR can lead to the activation of HSF4 as part of the cellular effort to restore normal function by enhancing the production of molecular chaperones. | ||||||
Bortezomib | 179324-69-7 | sc-217785 sc-217785A | 2.5 mg 25 mg | $135.00 $1085.00 | 115 | |
Bortezomib is a proteasome inhibitor that causes the accumulation of ubiquitinated proteins, thereby inducing a stress response that can activate HSF4 to address the heightened need for protein quality control mechanisms. | ||||||