AMP-PCP is an ATP analogue and can bind toHsp90N-terminal domain with aKdvalue of 3.8μM. AMP-PCP binding favors the formation of the active homodimer ofHsp90.
Cucurbitacin D is an active component inCucurbita texana, disrupts interactions betweenHsp90 and two co-chaperones, Cdc37 and p23. Cucurbitacin D prevents Hsp90 client (Her2, Raf, Cdk6, pAkt) maturation without induction of t...
Teprenone, an acylic polyisoprenoid, that is known as tetraprenylacetone or geranylgeranylacetone, is an anti-ulcer drug, clinically used for gastritis.
AMP-PCP disodium is an ATP analogue and can bind toHsp90N-terminal domain with aKdvalue of 3.8μM. AMP-PCP disodium binding favors the formation of the active homodimer ofHsp90.
10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of theheat shock response. 10,11-Dehydrocurvularin inhibitsTGF-β signallingpathway. Anti-tumorous activity.
Falcarinol (Panaxynol) is a natural, orally activeHsp90inhibitor targeting both the N-terminal and C-terminal of Hsp90 with limited toxicities. Falcarinol (Panaxynol) inducesapoptosis.
Feretoside, a phenolic compound extracted from the barks ofE. ulmoides, is aHSP inducerwhich act as cytoprotective agent.
Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.
3-Phenyltoxoflavin, a derivative of Toxoflavin, is anHsp90inhibitor, with aKdof 585nM for the interaction of Hsp90-TPR2A. 3-Phenyltoxoflavin has anti-cancer activity.
Pifithrin-μ is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
Tanespimycin (17-AAG) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Phase 2.
17-AEP-GA, anHSP90antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.
Rocaglamide (Roc-A) is isolated from the genusAglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor ofNF-κBactivation in T-cells. Rocaglamide is a potent and se...
ML346 is an activator ofHsp70 expression and HSF-1 activity, with an EC50 of 4.6μM for Hsp70. ML346 restores protein folding in conformational disease models, without significant cytotoxicity or lack of specificity. ML346 ind...
MKT-077 is a newly synthesized, highly water-soluble rhodacyanine dye that exhibits significant antitumor activity in a variety of model systems.
Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potentHsp90activator and enhances the Hsp90 molecular ch...
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