ACY-241

ACY-241 is an inhibitor of histone deacetylase 6 (HDAC6; IC₅₀ = 2.6 nM).¹ It is selective for HDAC6 over HDAC1-3, HDAC7, and HDAC9 (IC₅₀s = 35, 45, 46, 7,300, and 137 nM, respectively), as well as HDAC4, HDAC5, and HDAC9 (IC₅₀ = >20,000 nM for all). It reduces proliferation of A2780, TOV-21G, and MDA-MB-231 cells when used at a concentration of 3 µM and completely inhibits it and induces apoptosis at a concentration of 10 µM. ACY-241, when used in combination with paclitaxel (Item No. 10461), inhibits proliferation in MiaPaCa-2, TOV-21G, and T47D cells. It also reduces tumor growth in a MiaPaCa-2 mouse xenograft model when administered at a dose of 50 mg/kg in combination with paclitaxel. ACY-241, in combination with the somatostatin receptor agonist pasireotide (Item No. 24092), reduces hepatorenal cystogenesis in a rat model of polycystic liver disease.²

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1. Huang, P., Almeciga-Pinto, I., Jarpe, M., et al. Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models. Oncotarget 8(2), 2694-2707 (2017).

2. Lorenzo Pisarello, M., Masyuk, T.V., Gradilone, S.A., et al. The combination of an HDAC6 inhibitor and a somatostatin receptor agonist synergistically reduces hepato-renal cystogenesis in an animal model of polycystic liver disease. Am. J. Pathol. 188(4), 981-994 (2018).