4-Iodo-SAHA

4-iodo-SAHA is a hydrophobic derivative of the class I and class II HDAC (histone deacetylase) inhibitor SAHA. At 1 μM it demonstrates >60% inhibition of HDAC1 and HDAC6 activity in a deacetylase activity assay, similar to that of SAHA. 4-iodo-SAHA inhibits proliferation of SK-BR-3 breast-derived cell lines, HT29 colon-derived cell lines, leukemia-derived U937 tumor cell line, JA16, HL60 and K562 cell lines with EC50 values of 1.1 μM, 0.95 μM, 0.12 μM, 0.24 μM, 0.85 μM and 1.3 μM, respectively. It is 10-fold more potent as an inhibitor of U937 leukemia cell proliferation compared to SAHA.