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Neuromics

Small Compound/Modulator · Modulator

Romidepsin (FK-228)

Description

A potent and selective inhibitor of class I histone deacetylases (HDACs),  IC50 = 36, 47, 510 and 14,000 nM for HDAC1, 2, 4 and HDAC6, respectively [1]. Induces apoptosis in a variety of cell lines [2] and displays antitumor activity in mouse models [3]. Recently approved for clinical use in T-cell lymphoma [4].

References:

1) Furumai et al. (2002), FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases;  Cancer Res.., 62 4916

2) Panicker et al. (2010), Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells;  Cell Cycle, 9 1830

3) Ueda et al. (1994), FR901228, a novel anti-tumor bicyclic depsipeptide produced by Chromobacterium violaceum No. 968. III. Antitumor activities on experimental tumors in mice;  J. Antibiot. (Tokyo), 47 315

4) VanderMolin et al. (2011), Romodepsin (Istodax, NSC 630176, FR901228, FK228, depsipeptide): a natural product recently approved for cutaneous T-cell lymphoma;  J. Antibiotic. (Tokyo), 64 525

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For research use only. Not for diagnostic or clinical use.