Definition

An orally bioavailable fluorobisamide and heat shock factor 1 (HSF1) pathway inhibitor, with potential antineoplastic activity. Upon oral administration, HSF1 pathway inhibitor NXP800 targets and inhibits the activity of the HSF1-regulated pathway, thereby preventing HSF1-mediated transcription. This inhibits proliferation, migration, survival, and metastasis in susceptible tumor cells, especially in AT-rich interaction domain 1A (ARID1A)-mutated cancer cells. HSF1, a stress-inducible transcription factor that plays a key role in the transcriptional activation of the eukaryotic heat shock response; its activation leads to expression of many heat shock proteins (HSPs). Overexpressed, amplified and/or overactivated in many cancer cells, HSF1 activates a set of genes that play a key role in tumor initiation, progression and metastasis.