AES-350 是一种有效的口服活性 HDAC6 抑制剂，IC50 和 Ki 分别为 0.0244 μM 和 0.035 μM。 AES-350 在酶活性测定中也能对抗 HDAC3、HDAC8，IC50 值分别为 0.187 μM 和 0.245 μM。 AES-350 通过抑制 HDAC 触发 AML 细胞凋亡，可用于急性髓性白血病 (AML) 研究。
货号:ajcx24590
CAS:847249-57-4
分子式:C18H20N2O3
分子量：312.4
溶解度:DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml,Ethanol: 1 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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).¹It 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)