4-Iodo Suberoylanilide HydroxaMic Acid

Uses

A SAHA derivative with antiproliferative activity in several human cancer cell lines. Antitumor agent.

Biological Activity

4-iodo-saha is a hydrophobic derivative of saha, the class i and class ii histone deacetylase (hdac) inhibitor [1].the reversible acetylation of lysine residues in histone plays an important role in transcriptional activation and repression. the regulation of these post-translational modifications is balanced by histone acetyltransferase (hat) and histone deacetylase (hdac) activities. hdacs are also involved in reversible acetylation of non-histone proteins [1].4-iodo-saha is a histone deacetylase (hdac) inhibitor. in skbr3-breast-derived cell line, 4-iodo-saha inhibited cell proliferation with ec50 value of 1.1 μm. in ht29 colon-derived cell line, leukemia-derived u937 tumor cell line, ja16, hl60 and k562 cell lines, 4-iodo-saha inhibited cell proliferation with ec50 values of 0.95, 0.12, 0.24, 0.85 and 1.3 μm, respectively. 4-iodo-saha is 10-fold more potent as an inhibitor of u937 leukemia cell proliferation compared to saha (0.12 μm versus 1.2 μm). in skbr3 cells, 4-iodo-saha reduced acetylated h4 and p21 levels [1].

in vivo

References

[1]. salmi-smail c, fabre a, dequiedt f, et al. modified cap group suberoylanilide hydroxamic acid histone deacetylase inhibitor derivatives reveal improved selective antileukemic activity. j med chem. 2010 apr 22;53(8):3038-47.