Epoxomicin is a Selective and Irreversible Inhibitor of Proteasome

Epoxomicin (BU-4061T) is a potent, selective and irreversible proteasome inhibitor. Epoxomicin can cross the blood-brain barrier and has strongly antitumor and anti-inflammatory activity. Proteasome is a 700 kDa, cylindrical-shaped multicatalytic protease complex. It has 28 subunits and organizes into four rings. Besides, Eukaryote 20S proteasome has three major proteolytic...

5-Azacytidine, a Nucleoside Analogue of Cytidine, Inhibits DNA Methylation

In the mammalian genome, DNA methylation is an epigenetic mechanism involving the transfer of a methyl group onto the C5 position of the cytosine to form 5-methylcytosine. DNA methylation regulates gene expression by recruiting proteins involved in gene repression or by inhibiting the binding of transcription factor(s) to DNA....

Pimasertib is a Highly Selective and ATP non-Competitive Allosteric Inhibitor of MEK1/2

The RAS/RAF/MEK/MAPK and the PTEN/PI3K/AKT/mTOR pathways are key regulators of proliferation and survival in human cancer cells. RAF is a serine/threonine kinase that activates downstream signals in response to activated GTP-bound RAS by phosphorylating MEK  (MEK1 and MEK2). They in turn phosphorylate and activate MAPK (or ERK1 and ERK2)....

Epothilone B is a Microtubule Stabilizer

Microtubules are polymers of tubulin, which is one of several members of a small family of globular proteins. The tubulin superfamily includes five distinct families, the α-, β-, γ-, δ-, and ε-tubulins and a sixth family which is present only in kinetoplastid protozoa. The most common members α-tubulin and...

Bisantrene, an Antitumor Drug, Targets Eukaryotic Type II Topoisomerases

ImprotDNA topoisomerases are enzymes that disentangle the topological problems that arise in double-stranded DNA. Type II topoisomerases are ubiquitous enzymes that play essential roles in a number of fundamental DNA processes. Besides, Type II topoisomerases change DNA topology by generating transient DNA double strand breaks. Mammalian cells have two...

Splitomicin is a cell-permeable, potent SIR2 Inhibitor

The class III histone deacetylases (HDAC) are also known as the sirtuins. They are a member of the sirtuin family of proteins (SIRT1~7) and homologs of Sir2 (Sir2p) in yeast. SIRT1 shares a domain of about 275 amino acids with other sirtuins. It uses NAD+ to mediate the deacetylation...

Embelin is a Nonpeptidic XIAP Inhibitor

Embelin is an inhibitor of X-linked inhibitor of apoptosis protein (XIAP). It derives from the fruit of Embelia ribes. Embelin also possess therapeutic properties, such as anticancer, antioxidant, anti-inflammation, antidiabetes, and antihelminthic qualities.   XIAP is the most potent member of the inhibitors of apoptosis proteins (IAP) gene family....