HDAC Inhibitors

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Zolinza

Zolinza (Vorinostat, SAHA, suberoylanilide hydroxamic acid) is a histone deacetylase (HDAC) inhibitor that binds directly to the catalytic site of the enzyme thereby blocking substrate access. It inhibits class I and class II HDACs at nanomolar concentrations (IC50 < 86 nM).

Zolinza, SAHA

IUPAC Name: N-hydroxy-N'-phenyloctanediamide
Molecular Weight: 264.33 g/mol
Molecular Formula: C14H20N2O3
SMILES: ONC(=O)CCCCCCC(=O)Nc1ccccc1
Canonical SMILES: C1=CC=C(C=C1)NC(=O)CCCCCCC(=O)NO
InChIKey Identifier: WAEXFXRVDQXREF-UHFFFAOYSA-N
CAS Number: 149647-78-9
Melting point: 162-164 °C
Solubility: soluble in organic solvents such as ethanol, DMSO and DMF.
2D Molfile: Get the molfile
Synonyms: N1-hydroxy-N8-phenyl-octanediamide, SAHA, Suberoylanilide Hydroxamic Acid, Zolinza, Vorinostat

Zolinza is a drug used to treat a type of cancer called cutaneous T-cell lymphoma, also called CTCL. Zolinza is used in patients when the CTCL gets worse, does not go away, or comes back after treatment with other medicines.

CTCL, a type of non-Hodgkin's lymphoma, is a slow-growing form of cancer in which some of the body's white blood cells known as T-lymphocytes or T-cells become malignant. Normal T-cells function by regulating the body's immune system in its job of fighting infections and other foreign antigens. In CTCL, the malignant T-cells are drawn to the skin, where some are deposited.

References:
1) Marks, P.A., Breslow, R. Dimethyl sulfoxide to vorinostat: Development of this histone deacetylase inhibitor as an anticancer drug. Nature Biotechnology 25(1) 84-90 (2007).
2) Tan J, Cang S, Ma Y, Petrillo RL, Liu D. Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents. J Hematol Oncol. 2010 Feb 4;3(1):5.
3) Lane AA, Chabner BA. Histone deacetylase inhibitors in cancer therapy. J Clin Oncol. 2009 Nov 10;27(32):5459-68.

HDACs


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