HDAC Inhibitors

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CI-994 (Tacedinaline; PD-123654; GOE-5549; Acetyldinaline) is a novel orally active compound with a wide spectrum of antitumor activity in preclinical models, in vitro and in vivo. The mechanism of action of CI-994 is not entirely understood but it has been shown to inhibit HDAC-1 and HDAC-2 and cellular proliferation.

CI-994 originally was developed as an anticonvulsant agent and later was reported to have antitumor activity.


IUPAC Name: 4-(acetylamino)-N-(2-aminophenyl)benzamide
Molecular Weight: 269.31 g/mol
Molecular Formula: C15H15N3O2
SMILES: c2cc(NC(=O)C)ccc2C(=O)Nc1ccccc1N
Canonical SMILES: CC(=O)NC1=CC=C(C=C1)C(=O)NC2=CC=CC=C2N
CAS Number: 112522-64-2
Melting point: 207-208 °C
Solubility: DMSO - 10 mg/mL
2D Molfile: Get the molfile
Synonyms: Tacedinaline, PD-123654, GOE-5549, Acetyldinaline

A randomised, double-blind Phase II study has been performed comparing CI-994 plus gemcitabine vs. gemcitabine plus placebo and published results are awaited.

1) S. Shore et al. Chemotherapy for Pancreatic Cancer: Chemotherapy Agents in Advanced Pancreatic Cancer. Alimentary Pharmacology & Therapeutics. 2003;18(11).
2) Alan J. Kraker et al. Modulation of Histone Acetylation by [4-(Acetylamino)-N-(2-Amino-phenyl) Benzamide] in HCT-8 Colon Carcinoma. Mol Cancer Ther April 2003 2; 401
3) Loprevite M et al. In vitro study of CI-994, a histone deacetylase inhibitor, in non-small cell lung cancer cell lines. Oncol Res. 2005;15(1):39-48.
4) Richards D, Waterhouse D, Wagener DJT, et al. Randomised, double blind, placebo controlled phase II study of the histone deacetylase inhibitor C1-994 plus gemcitabine (C1-994+G) in the treatment of patients with advanced pancreatic cancer (APC). Proc ASCO Abstract 644.


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