14513-15-6

Cambinol has been used:

• as an inhibitor of sirutins (SIRT1 and 2) in hepatocarcinoma cell lines to test its effect on cellular viability and colony formation
• as a SIRT1 and SIRT2 inhibitor to test its effect on frizzled 7 (FZD7) expression in the breast cancer cells MDA-MB-231 and T-47D cells
• as a sirutin inhibitor in L929 cells to test its protective effect against tumor necrosis factor (TNF)-induced cell death

SIRT1/2 Inhibitor IV, Cambinol is an inhibitor of SIRT1, SIRT2, and SIRT5.

sirt1/2 inhibitor iv (cambinol) is a small-molecule inhibitor of sirt1 and sirt2 with ic50 values of 56 ?m and 59 ?m, respectively [1].sirtuin 1 (sirt1) and sirt2 are nad-dependent deacetylases and are members of sirtuin family protein. sirt1 regulate pathways in metabolism, inflammation and tumorigenesis and sirt2 functions as a tubulin deacetylase[2].sirt1/2 inhibitor iv is a cell-permeable sirt1 and sirt2 inhibitor. sirt1/2 inhibitor iv inhibited human sirt1 and sirt2 nad-dependent deacetylase activity with ic50 values of 56 and 59 ?mol/l, respectively. in nci h460 lung cancer cell line, combined inhibition of sirt2 and hdac6 with sirt1/2 inhibitor iv and trichostatin a resulted in hyperacetylation of tubulin. sirt1/2 inhibitor iv also increased acetylation of p53. in p53-positive lung cancer cell line nci h460, sirt1/2 inhibitor iv mediated inhibition of sirt1 sensitized cells to etoposide in p53-independent manner [1].in a mouse xenograft model, sirt1/2 inhibitor iv (100 mg/kg) administered i.v. into the tail vein or i.p. daily for 2 weeks (five injections per week) reduced tumor growth [1]. in mice pre-treated with cambinol for 2 hours and then exposed to 6% oxygen for 6 hours, cambinol significantly reduced epo mrna in the kidney and the liver [2].

Cambinol is a Sirtuin (Human Silent Information Regulator) Type 1/2 Inhibitor. Sirtuins are structurally and mechanistically unrelated to HDACs Class 1 & 2 deacetylases but share many protein targets. HDAC is a large complex enzyme family involved in epigenetic-control of gene expression. Sirt2 has an IC50 equal to 59 μM.

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heltweg b, gatbonton t, schuler ad, et al. antitumor activity of a small-molecule inhibitor of human silent information regulator 2 enzymes. cancer res. 2006 apr 15;66(8):4368-77.laemmle a, lechleiter a, roh v, et al. inhibition of sirt1 impairs the accumulation and transcriptional activity of hif-1α protein under hypoxic conditions. plos one. 2012;7(3):e33433.