Tag: HDAC

Spiruchostatin A is a Potent HDAC Inhibitor with anticancer activity

Histone deacetylase (HDAC) is an enzyme that catalyzes the removal of acetyl functional groups from the lysine residues of histones and non-histones. Among other things, histone lysine acetylation is highly reversible.  HDAC-catalyzed epigenetic modification of histone acetylation regulates chromatin structure and transcription, while non-histone deacetylation controls a variety of...

Abexinostat is an Orally Available Pan-HDAC Inhibitor

HDAC (Histone deacetylases) are a class of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone. To date, There are 18 human HDACs. Besides, HDACs include four classes on the basis of their homology with yeast proteins. Class I HDACs (HDAC1, 2, 3, and...

Trichostatin A (TSA) is a Specific Inhibitor of HDAC Class I/II

Histone deacetylases (HDACs) are enzymes that remove acetyl groups from histone and non-histone proteins. To date, 18 different mammalian HDACs have been identified and divided into four classes: the Class I Rpd3-like proteins (HDAC1, HDAC2, HDAC3, and HDAC8); the Class II Hda1-like proteins (HDAC4, HDAC5, HDAC6, HDAC7, HDAC9, and...

AES-135 is a Potent HDAC Inhibitor

Pancreatic cancer is cancer that’s found anywhere in the pancreas. Histone deacetylases (HDACs) regulate the post-translational modification of histones and consequent gene expression. HDACs act as transcriptional repressors and overexpress in several types of cancer, including pancreatic cancer. HDAC inhibitors are effective in killing pancreatic cancer cells. In this...

CXD101 is a Selective and Orally Active Class I HDAC Inhibitor

Aberrant expression of classical HDACs associates with a variety of malignancies, including solid and hematological tumors. HDACs have also been found broadly dysregulated in multiple myeloma (MM). In particular, the mechanisms that HDACs regulate tumorigenesis are quite diverse. HDACs induce a range of cellular and molecular effects through the...

Triciferol is Both a VDR Agonist and HDAC Antagonist

The biologically active metabolite of vitamin D3, 1α,25-dihydroxyvitamin D3 (1,25D), is a primary regulator of calcium homeostasis. 1,25D also controls cell differentiation and proliferation through binding to the nuclear vitamin D receptor (VDR). It regulates histone acetylation, chromatin remodeling, and recruitment of RNA polymerase II and ancillary factors required...