Tenovin-6 CAS NO.1011557-82-6

tenovin-6 is the water soluble analog of tenovin-1 (hy-13423) and acts as a potent sirt1 (ic50=21 um) and sirt2 (ic50= 10 um) inhibitor as well as p53 activator.
ic50 value: 21 um (human sirt1); 10 um (human sirt2) [1]
target: sirt1; sirt2
in vitro: tenovin-6 inhibits the growth of s. cerevisiae cultures with an ic50 of 30 μm and is more toxic to yeast than the less water-soluble tenovin-1. tenovin-6 decreases purified human sirt1 peptide deacetylase activity in vitro with an ic50 of 21 μm and human sirt2 activity with an ic50 of 10 μm. inhibition of sirt3 by tenovin-6 in this assay was significantly lower with an ic50 of 67 μm.tenovin-6 does not inhibit enzymatic assays in general as the activity of a panel of 51 purified kinases was not significantly affected [1]. kiaa1967 expression is differentially downregulated in pdac and impacts on the sensitivity of pdac cells to the sirt1/2 inhibitor tenovin-6 [2]. in chronic lymphocytic leukemia (cll) cells, tnv-6 causes non-genotoxic cytotoxicity, without adversely affecting human clonogenic hematopoietic progenitors in vitro, or murine hematopoiesis. mechanistically, exposure of cll cells to tnv-6 did not induce cellular apoptosis or p53-pathway activity [3].
in vivo: tenovin-6 was administered daily at 50 mg/kg by intraperitoneal injection. control animals were treated with vehicle solution containing cyclodextrin 20% (w/v) (cat. no. c0926 sigma) and dmso 10% (v/v). tumor diameters were measured using calipers, and volumes were calculated using the equation v = π4/3[(d1 + d2)/4]. median values of tumor size were calculated for each time point as well as the corresponding 95% confidence intervals [1].