Category: Cancer

VU0359595 is a Selective PLD1 Inhibitor

Phospholipase is a member of a very complex group of enzymes that break down phospholipids into fatty acids and other compounds. Phospholipase D (PLD) is an enzyme of the phospholipase superfamily. There are two mammalian isoforms of PLD, coined PLD1 and PLD2, and despite conserved regulatory and catalytic domains....

XL092 is a Potent Axl, Mer and C-Met kinase Inhibitor

Human Axl belongs to the TAM subfamily of receptor tyrosine kinases that includes Mer. TAM kinases contain two immunoglobulin-like domains and two fibronectin type III domains. Many cancer cells exhibit overexpressed Axl. And it is initially cloned from patients with chronic myelogenous leukemia. Axl has been associated with cancers...

Bestatin is a Broad-Spectrum, and Competitive Aminopeptidase Inhibitor

Aminopeptidases catalyze the cleavage of amino acids from the amino terminus of protein or peptide substrates. Regarding catalytic mechanism, most of the aminopeptidases are metallo-enzymes. In addition, aminopeptidase is widely present in animal and plant kingdomsis widely present in , found in many subcellular organelles, in cytoplasm, and as...

Alda-1 is a potent ALDH2 Agonist

Aldehyde dehydrogenase 2 (ALDH2) is ubiquitously found in various tissues, including the heart, brain, and skeletal muscle, and highly expressed in the mitochondria. Many cellular functions show relations with ALDH2. They include detoxification of aldehydes, cell survival, cell proliferation, and apoptosis. The deficiency of ALDH2 causes the accumulation of...

Zebularine is a DNA Methyltransferase Inhibitor

DNA methyltransferase (DNMT) family enzymes catalyze the transfer of methyl to DNA. Specifically, DNMT is a conserved cytosine methylase family, which plays a key role in epigenetic regulation. The DNMT family has four members, including DNMT1, Dnmt3a, DNMT3b, and DNMT3l. Different from other DNMTs, DNMT3l does not have any...

MRTX1133 is a Highly Selective, First-in-Class Inhibitor of KRAS G12D

Mutant KRAS is an attractive drug target for the treatment of a number of cancers for many decades. Until recently, the high affinity of KRAS for GDP/GTP and the lack of any other apparent binding pocket have significantly hampered the development of KRAS inhibitors. KRAS inhibitor relies on a...

A 83-01 is a Potent Inhibitor of TGF-β Type I Receptor ALK5 Kinase

TGF-β, activin, nodal, and bone morphogenetic proteins (BMPs) belong to the TGF-β superfamily. It regulates a wide range of cellular responses, including cell proliferation, differentiation, adhesion, migration, and apoptosis. TGF-β and related proteins transduce signals through two distinct serine/threonine kinase receptors, including type I and type II. The function...