17(S)-HDHA is a hydroxy fatty acid formed from docosahexaenoic acid (DHA, Cay-90310) by 15-lipoxygenase (15-LO) and is a precursor to 17(S)-resolvins. 17(S)-HDHA inhibits platelet 12-LO (IC50 = 0.4 µM). It inhibits TNF-alpha-induced expression of IL1B in a human glial cell line (IC50 = ~0.5 nM). 17(S)-HDHA (100 nM)...

EX-527 is an inhibitor of sirtuin 1 (SIRT1, IC50 = 0.098 µM). It is selective for SIRT1 over SIRT2, and SIRT3 (IC50s = 19.6 and 48.7 µM, respectively) and the cytochrome P450 (CYP) isoforms CYP3A4, CYP2D6, CYP2C9, CYP2C19, and CYP1A2 at 1 µM. EX-527 (50 µM) induces cell cycle arrest at the G1 phase in MCF-7...

Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1,...

Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC50s = ~100, ~100, ~100, and 300 nM for Cdk1, Cdk2, Cdk4, and Cdk7, respectively). It also inhibits TEFb, a complex composed of Cdk9 and cyclin T1, with a Ki value of 3 nM. Flavopiridol inhibits transcription of a CMV promoter in HeLa...

Phosphatidylcholine species are a common class of phospholipids that comprise the mammalian cell membrane. 1,2-Didecanoyl PC (DPC) is a synthetic, less hydrophobic phospholipid that has been found to be useful for enhancing the absorption of peptide drugs and hormones such as insulin. Thus, the bioavailability of...