General description

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 µM 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 µM, 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 µM) 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-α-induced NF-κB activity in HeLa or heat shock-induced HSF1 ser230 phosphorylation and promoter association in HCT-116 even at concentrations as high as 10 µM.

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 µM in HCT-116 ChIP assays), a critical step for heat shock-induced transcription activation (IC₅₀﹤1, ﹤3, ﹤5, and ﹤10 µM, 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 µM) and effectively suppress HCT-116-derived tumor growth in mice in vivo (50 mg/kg i.p.).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Yoon, Y.J., et al. 2010. J. Biol. Chem.286, 1737.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)