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Beschreibung

A cell-permeable 2,6-diaminopyridine compound that interacts with HSF1 (heat shock factor 1) in a reversible manner and prevents HSF1 from recruiting p-TEFb (positive transcription elongation factor b) to the hsp70 promoter site (IC50 <=3 µ,M in HCT-116 ChIP assays), a critical step for the p-TEFb CDK9 subunit-catalyzed pol II CTD (RNA polymerase II c-terminal domain) Ser-2 phosphorylation and transcription activation upon heat shock induction (IC50<1, <3, <5, and <10 µ,M, respectively, against reporter, HSP47, HSP27, and HSP70 transcription in HCT-116 cultures). Reported to exhibit antiproliferation activity against several cancer cultures in vitro (IC50 ranges from 3 to 8 µ,M) and effectively suppress HCT-116-derived tumor growth in mice in vivo (by 47.4% on day 31, single i.p. dosage of 50 mg/kg on day 13 after cancer implantation). Does not affect TNF-alpha-induced NF-kappaB activity in HeLa or heat shock-induced HSF1 ser230 phosphorylation and promoter association in HCT-116 even at concentrations as high as 10 µ,M., A cell-permeable 2,6-diaminopyridine compound that interacts with HSF1 in a reversible manner and prevents HSF1 from recruiting p-TEFb to the hsp70 promoter site (IC50 <=3 µ,M in HCT-116 ChIP assays), a critical step for heat shock-induced transcription activation (IC50<1, <3, <5, and <10 µ,M, respectively, against reporter, HSP47, HSP27, and HSP70 transcription in HCT-116 cultures). Reported to exhibit antiproliferation activity against several cancer cultures in vitro (IC50 from 3 to 8 µ,M) and effectively suppress HCT-116-derived tumor growth in mice in vivo (50 mg/kg i.p.).