MC2590, a Potent HDAC Inhibitor, inhibits HDAC1-3, -6, -8, and -10
Histone deacetylase (HDAC) is an epigenetic enzyme that regulates gene expression through histone deacetylation. It leads to more closed chromatin structure and gene expression inhibition. Many non-histones are also targets of HDAC, such as α Microtubulin, heat shock protein (HSP) 90, and hypoxia-inducible factor HIF-1 α. Specifically, HDAC is...
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...
Purinostat mesylate is a Selective HDAC Inhibitor With anti-Leukemia Effects
Purinostat mesylate is a selective inhibitor of HDAC. This compound inhibits class I and class IIb HDACs with IC50s from 0.81 to 11.5 nM. Purinostat mesylate (1-10 μM) inhibits HDAC1, 2, 3, and 8. And the IC50s are 0.81, 1.4, 1.7, and 3.8 nM, respectively. It also inhibits HDAC6 and 10,...
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...