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.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Yoon, Y.J., et al. 2010. J. Biol. Chem.286, 1737.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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The Journal of biological chemistry, 286(3), 1737-1747 (2010-11-17)
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