KNK437

KNK437 is a small molecule benzylidene lactam that functions as a potent inhibitor of the heat shock response. It specifically inhibits the induction and activity of Heat Shock Factor 1 (HSF1), the primary transcription factor responsible for the expression of heat shock proteins (HSPs) such as HSP70, HSP40, and HSP105. By blocking HSF1, KNK437 prevents cells from mounting a protective response to proteotoxic stress, hyperthermia, and certain chemotherapeutic agents. In the context of oncology, it has been shown to reverse chemotherapy resistance and inhibit aerobic glycolysis (the Warburg effect) in cancer cells, such as non-small cell lung cancer (NSCLC), often in combination with other agents like melittin or cisplatin. It is widely used as a pharmacological tool in preclinical research to study HSF1 signaling and thermotolerance.

Other names

N-formyl-3,4-methylenedioxybenzylidene-gamma-butyrolactam