An inhibitor of class I and class IIb HDACs
AES-350 is an inhibitor of class I histone deacetylases (HDACs; IC50s = 0.605, 0.187, and 0.245 µM for HDAC1, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.0244 and 0.899 µM for HDAC6 and HDAC10, respectively).1 It is selective for class I and class IIb HDACs over HDAC2, -4, -5, -7, -9, and -11 (IC50s = >1 µM for all). AES-350 is cytotoxic to MV4-11, MOLM-13, and MRC-9 cells (IC50s = 0.576, 6, and 33.2 µM, respectively). It induces apoptosis in MV4-11 cells in a concentration-dependent manner.
1.Shouksmith, A.E., Gawel, J.M., Nawar, N., et al.Class I/IIb-selective HDAC inhibitor exhibits oral bioavailability and therapeutic efficacy in acute myeloid leukemiaACS Med. Chem. Lett.11(1)56-64(2019)
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