Inauhzin

Inauhzin is a cell-permeable, SIRT1 inhibitor (IC₅₀ = 0.7-2 µM) that reactivates p53 by inhibiting SIRT1 deacetylation activity.¹ It binds directly to SIRT1 and does not affect SIRT2, SIRT3, or HDAC8.¹ Inauhzin has been shown to inhibit cell proliferation by inducing p53-dependent apoptosis in various human cancer cells (IC₅₀s = 5.4, 51.9, 3.2, 33.9, and 85.4 µM for H460, H1299, A549, HT-29, and WI38 cells, respectively), as well as in xenograft tumors derived from H460 cells.¹ It has also been shown to activate p53 synergistically with the Mdm2 inhibitor nutlin-3 (Item No. 10004372), sensitizing cancer cells to cisplatin (Item No. 13119) and doxorubicin (Item No. 15007).²

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1. Zhang, Q., Zeng, S.X., Zhang, Y., et al. A small molecule Inauhzin inhibits SIRT1 activity and suppresses tumour growth through activation of p53. EMBO Mol. Med. 4(4), 298-312 (2012).

2. Zhang, Y., Zhang, Q., Zeng, S.X., et al. Inauhzin and Nutlin3 synergistically activate p53 and suppress tumor growth. Cancer Biol. Ther. 13(10), 915-924 (2012).