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Anticancer molecular libraries

HDAC inhibitor library

(HDAC = Histone deacetylases  )

Histone deacetylase inhibitors (HDAC inhibitors, HDI) are a class of compounds that interfere with the function of histone deacetylase. Also in recent years, there has been an effort to develop HDIs as a cancer treatment or adjunct The exact mechanisms by which the compounds may work are unclear, but epigenetic pathways are proposed. Richon et al. found that HDAC inhibitors can induce p21 (WAF1) expression, a regulator of p53's tumor suppressor activity. HDACs are involved in the pathway by which the retinoblastoma protein (pRb) suppresses cell proliferation. The pRb protein is part of a complex that attracts HDACs to the chromatin so that it will deacetylate histones. HDAC1 negatively regulates the cardiovascular transcription factor Kruppel-like factor 5 through direct interaction. Estrogen is well-established as a mitogenic factor implicated in the tumorigenesis and progression of breast cancer via its binding to the estrogen receptor alpha (ERα). Recent data indicate that chromatin inactivation mediated by HDAC and DNA methylation is a critical component of ERα silencing in human breast cancer cells.  (soruce: http://en.wikipedia.org/wiki/Histone_deacetylase_inhibitor).

The following compounds are HDAC inhibitors which are approved or in clinical trials:
* Vorinostat was licenced by the U.S. FDA in October 2006 for the treatment of cutaneous T cell lymphoma (CTCL).
* Romidepsin (trade name Istodax) was licenced by the US FDA in Nov 2009 for cutaneous T-cell lymphoma (CTCL),
* Panobinostat is in clinical trials for various cancers including a phase III trial for cutaneous T cell lymphoma (CTCL).
* Valproic acid is under investigation for various cancers including leukemia.
* Mocetinostat (MGCD0103) is undergoing clinical trials for treatment of various cancers (including follicular lymphoma, Hodgkin lymphoma and acute myeloid leukemia).
* Belinostat has had a phase II trial for relapsed ovarian cancer.
* PCI-24781 has started a phase II trial for sarcoma, and another for lymphoma.
* AR-42  has started clinical trials in 2010 for various cancers (relapsed or treatment-resistant multiple myeloma, chronic lymphocytic leukemia or lymphoma).
* CUDC-101 intended for cancer, has started clinical trials, it also inhibits EGFR and HER2.

Selected HDAC inhibitors approved or in clinical trials

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