FKBP52 Activators
FKBP52 Activators are diverse chemical compounds that enhance the functional activity of FKBP52 through various biochemical mechanisms. FK506 (Tacrolimus) and Rapamycin (Sirolimus) are immunophilins that bind directly to FKBP52, which could augment its intrinsic peptidyl-prolyl isomerase activity, crucial for protein folding and enhancing steroid hormone receptor complex formation and function. Mifepristone, a synthetic steroid, interacts with the glucocorticoid receptor and may increase FKBP52's chaperone efficiency, leading to an elevated receptor-FKBP52 interaction and nuclear translocation, pivotal for hormone signaling. Geldanamycin and 17-AAG, both Hsp90 inhibitors, possibly elevate FKBP52's activity by altering the composition of the Hsp90 co-chaperone complex, while Deoxyspergualin's interaction with Hsp70 may indirectly boost the FKBP52-linked chaperone network, thus enhancing FKBP52's role in receptor regulation.
Furthermore, Phenylarsine Oxide, through inhibition of PTPFKBP52 Activators encompass a range of chemical compounds that specifically enhance the biochemical activity of FKBP52, influencing cellular processes through various signaling pathways. FK506, also known as Tacrolimus, binds to and enhances the peptidyl-prolyl isomerase activity of FKBP52, which is crucial for the proper folding and function of steroid hormone receptors. This interaction facilitates the transport of the receptor complex into the nucleus, intensifying its transcriptional activity. Similarly, Rapamycin, though primarily an mTOR pathway inhibitor, can increase FKBP52's chaperone activity on steroid hormone receptors by altering its protein interactions, which may indirectly promote FKBP52's function. Mifepristone, by engaging with the glucocorticoid receptor, causes increased formation of the receptor-FKBP52 complex, thereby promoting its nuclear translocation and signaling. Geldanamycin and 17-AAG, which target Hsp90, may disrupt the Hsp90-cochaperone complex and consequently enhance the availability and activity of FKBP52 with steroid hormone receptors.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
FK-506 | 104987-11-3 | sc-24649 sc-24649A | 5 mg 10 mg | $78.00 $151.00 | 9 | |
Tacrolimus binds to FKBP52 and potentiates its peptidyl-prolyl isomerase activity, which is essential in protein folding and contributes to its high-affinity binding to steroid hormone receptors, thus enhancing the receptor complex's transport into the nucleus. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $63.00 $158.00 $326.00 | 233 | |
Rapamycin binds to FKBP52 and inhibits the mammalian target of rapamycin (mTOR) signaling pathway. Although primarily known as an inhibitor, this binding can increase FKBP52's interaction with other proteins and may facilitate its chaperone activity on steroid hormone receptors. | ||||||
Mifepristone | 84371-65-3 | sc-203134 | 100 mg | $61.00 | 17 | |
Mifepristone enhances the chaperone activity of FKBP52 by acting on the glucocorticoid receptor, leading to an increased receptor-FKBP52 complex formation and promoting nuclear translocation, which is crucial for receptor-mediated signaling. | ||||||
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 Hsp90, a known co-chaperone with FKBP52. This interaction can alter the Hsp90 co-chaperone complex, potentially enhancing the availability of FKBP52 to interact with steroid hormone receptors. | ||||||
17-AAG | 75747-14-7 | sc-200641 sc-200641A | 1 mg 5 mg | $67.00 $156.00 | 16 | |
17-AAG binds to Hsp90, potentially increasing the chaperone activity of FKBP52 by modulating the Hsp90/FKBP52 complex dynamics, leading to enhanced steroid receptor signaling. | ||||||
Phenylarsine oxide | 637-03-6 | sc-3521 | 250 mg | $41.00 | 4 | |
Phenylarsine Oxide inhibits the function of PTPases, which can increase tyrosine phosphorylation levels that may indirectly enhance the chaperone activity of FKBP52 in receptor complexes. | ||||||
Dimethyl Sulfoxide (DMSO) | 67-68-5 | sc-202581 sc-202581A sc-202581B | 100 ml 500 ml 4 L | $31.00 $117.00 $918.00 | 136 | |
DMSO can induce conformational changes in proteins and might enhance the chaperone activity of FKBP52 by stabilizing receptor-FKBP52 complexes. | ||||||
Cycloheximide | 66-81-9 | sc-3508B sc-3508 sc-3508A | 100 mg 1 g 5 g | $41.00 $84.00 $275.00 | 127 | |
Cycloheximide inhibits eukaryotic protein synthesis and can thereby increase the relative activity of existing chaperone proteins like FKBP52 by reducing competition for client proteins. | ||||||
Withaferin A | 5119-48-2 | sc-200381 sc-200381A sc-200381B sc-200381C | 1 mg 10 mg 100 mg 1 g | $130.00 $583.00 $4172.00 $20506.00 | 20 | |
Withaferin A binds to Hsp90, which could modify the chaperone complex that includes FKBP52, enhancing its activity with steroid hormone receptors. | ||||||
Celastrol, Celastrus scandens | 34157-83-0 | sc-202534 | 10 mg | $158.00 | 6 | |
Celastrol induces heat shock response and could potentiate the chaperone activity of FKBP52 by upregulating the expression of heat shock proteins and co-chaperones, thus reinforcing the chaperone network that FKBP52 is a part of. | ||||||