Protein Information

Name heat shock factor 1
Synonyms HSF 1; HSTF1; HSF1; HSTF 1; Heat shock factor protein 1; Heat shock transcription factor 1; Heat shock factor 1; Heat shock factor protein 1s…

Compound Information

Name rotenone
CAS

Reference List

PubMed Abstract RScore(About this table)
19502057 Zhou Y, Wei L, Brady TP, Murali Mohan Redddy PS, Nguyen T, Chen J, Au Q, Yoon IS, Yip G, Zhang B, Barber JR, Ng SC: Pyrimido [5,4-e][1,2,4] triazine-5,7 (1H,6H)-dione derivatives as novel small molecule chaperone amplifiers. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4303-7. Epub 2009 May 27.

Lead optimization led to the discovery of compound 4A-13, which displayed potent HSF1 activity under mild heat stress (EC (50)=2.5microM) and significant cytoprotection in both rotenone (EC (50)=0.23microM) and oxygen-glucose deprivation cell toxicity models (80% protection at 2.5microM).
7(0,0,1,2) Details
19015292 Au Q, Kanchanastit P, Barber JR, Ng SC, Zhang B: High-content image-based screening for small-molecule chaperone amplifiers in heat shock. J Biomol Screen. 2008 Dec;13(10):953-9. Epub 2008 Nov 17.

The expression of many heat shock proteins is controlled by HSF1, which forms stress granules in the nucleus when transcriptionally activated.
Treatment of cells with selected hits exhibited significant cytoprotection from both oxygen glucose deprivation and rotenone-induced stresses.
3(0,0,0,3) Details