KRIBB11 is an inhibitor of Heat shock factor 1 (HSF1), with IC50 of 1.2 uM.
CAS：342639-96-7
分子式：C13H12N6O2
分子量：284.27
纯度：98%
存储：Store at -20°C

Background:

KRIBB11 is an inhibitor of Heat shock factor 1 (HSF1), with IC50 of 1.2 uM.

KRIBB11 blocks the induction of HSF1 downstream target proteins such as HSP27 and HSP70. KRIBB11 induces growth arrest and apoptosis of HCT-116 cells. KRIBB11 inhibits HSF1-dependent recruitment of p-TEFb (positive transcription elongation factor b) to the hsp70 promoter[1]. PARP and caspase-3 cleavage is increased in cells treated with KRIBB11. Incubating RKO with KRIBB11, shows a toxic threshold of about 10 uM, and an IC50 of 20-30 uM[2].

KRIBB11 (50 mg/kg, i.p.) results in a 47.4% inhibition of tumor growth in nude mice, without body weight loss[1].

参考文献:
[1]. Yoon YJ, et al. KRIBB11 inhibits HSP70 synthesis through inhibition of heat shock factor 1 function by impairing the recruitment of positive transcription elongation factor b to the hsp70 promoter. J Biol Chem. 2011 Jan 21;286(3):1737-47.
[2]. Samarasinghe B, et al. Heat shock factor 1 confers resistance to Hsp90 inhibitors through p62/SQSTM1 expression and promotion of autophagic flux. Biochem Pharmacol. 2014 Feb 1;87(3):445-55.