3-(1-Methyl-4-phenylacetyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide

Description

APHA compound 8 is an inhibitor of class I histone deacetylases (HDACs; IC₅₀s = 3.7, 7.4, 0.42, and 2.8 μM for HDAC1, -2, -3, and -8, respectively) as well as class II HDACs (IC₅₀s = 3.1, 0.1, 3.1, and 4.2 μM for HDAC4, -6, -7, and -10, respectively). It is selective for class I and II HDACs over class III HDACs (IC₅₀s = >30 μM for SIRT1, SIRT2, and SIRT3) and the histone acetyltransferase PCAF (IC₅₀ = >30 μM). At 48 hours post-infection, APHA compound 8 increases replication of oncolytic herpes simplex virus (oHSV) in MDA-MB-231 and 4T1 breast cancer cells when used prior to viral infection at concentrations of 10 and 50 μM.

Uses

HDAC-IN-69 (Compound 2) is a derivative of an HDAC inhibitor with inhibitory activity targeting maize histone deacetylase HD2[1].

IC 50

HD2

References

[1] Ragno R, et al. 3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies. J Med Chem. 2004 Mar 11;47(6):1351-9. DOI:10.1021/jm031036f