[HTML][HTML] KRIBB11 inhibits HSP70 synthesis through inhibition of heat shock factor 1 function by impairing the recruitment of positive transcription elongation factor b to …

YJ Yoon, JA Kim, KD Shin, DS Shin, YM Han… - Journal of Biological …, 2011 - ASBMB
Heat shock factor 1 (HSF1) is the master switch for heat shock protein (HSP) expression in
eukaryotes. A synthetic chemical library was screened to identify inhibitors of HSF1 using a
luciferase reporter under the control of a heat shock element. A compound named KRIBB11
(N 2-(1H-indazole-5-yl)-N 6-methyl-3-nitropyridine-2, 6-diamine) was identified for its activity
in abolishing the heat shock-induced luciferase activity with an IC 50 of 1.2 μmol/liter. When
the cells were exposed to heat shock in the presence of KRIBB11, the induction of HSF1 …