KRIBB11 is an inhibitor of heat shock factor 1 (Hsf1) with an IC50 value of 1.2 ?M in a luciferase reporter assay.{37149} It blocks heat shock-induced Hsp70, Hsp40, and Hsp27 mRNA expression and down-regulates protein expression of the Hsf1 target proteins Hsp70 and Hsp27 in HCT116 cells in a dose-dependent manner. KRIBB11 specifically binds to Hsf1 over other Hsf1-associated proteins, lacking activity at heat shock protein 90 (Hsp90), Hsf2, and Cdk9 in an in vitro pull-down assay. It inhibits growth of HCT116, Mia-PaCa-2, SW620, HT-29, A549, and MDA-MB-231 cancer cell lines (IC50s = 3-8 ?M) via induction of cell cycle arrest at the G2/M phase and apoptosis. In vivo, administration of KRIBB11 decreases tumor growth in a mouse HCT116 xenograft model. KRIB11 administration also attenuates dengue virus progression and reduces mortality without affecting bodyweight in infected mice.{37150}
5 mg
CAS number
Cayman Chemical
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