Tag: HDAC

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...

CHDI-390576 is a CNS Penetrant Class IIa HDAC Inhibitor

Class IIa HDAC is a transcriptional corepressor enzyme. They interact with MEF2 transcription factors and the N-CoR, BCoR, and CtBP corepressors.  They are capable of shuttling between the cytoplasm and nucleus, hence they are directly linked to cellular signaling networks. Class IIa HDACs found in a wide variety of...

CG-200745, a HDAC Inhibitor, Induces the Accumulation of p53

Histone deacetylase (HDAC) inhibits are considered to be promising agents that can be used as treatments for cancer. CG-200745 is a novel and potent hydroxamate-based pan-HDAC inhibitor. CG-200745 has the hydroxamic acid moiety to bind zinc at the bottom of the catalytic pocket. We will introduce its anti-tumorigenic property...

SS-208 is a Selective HDAC6 Inhibitor for Melanoma

Malignant melanoma represents the most aggressive and deadliest form of cutaneous cancer. This disease possesses the characteristic of increasing incidence, high metastasis, rapid disease progression, poor prognosis, and high mortality. The latest data showed that patients with metastatic melanoma have a poor prognosis with a 5-year survival rate of...