A cell-permeable 2,6-diaminopyridine compound that directly binds HSF1 and reversibly inhibits its transcriptional activity (IC50=1.2uM in heat shocked p[HSE]4-Ta-Luc transfected HCT-116 cells), and suppresses both the transcription and expression of hsp70, hsp47 and hsp27. Shown to block heat shock-induced p-TEFb (positive transcription elongation factor b) recruitment to the hsp70 promoter and inhibit the phosphorylation of RNA Pol II CTD-Ser2 with no effect on TNF-a-stimulated NF-kB activity in HeLa cells. Induces G2/M growth arrest and apoptosis (IC50 ~5uM in HCT-116 cells), and further decreases tumor growth in mouse xenograft regression model (50mg/kg, i.p.).
Formula:C13H12N6O2
Molecular Weight:284.3
Solubility:DMSO (50mg/ml)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
