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…
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…
Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. JAK includes JAK1, JAK2, JAK3 and TYK2. JAK serves as the…
The BTK kinases comprise 5 structural domains, including pleckstrin homology, TEC homology, Src homology, Src homology, and kinase domains. The activation of BTK kinase depends on recruitment to the plasma…
β-Lapachone is an ortho-naphthoquinone and inhibits topoisomerase I. β-Lapachone is a classic quinone-containing antitumor NQO1-bioactivatable drug that directly kills NQO1-overexpressing cancer cells. NQO1 is an antioxidative enzyme that helps recover…
PARP is a family of proteins involved in many cellular processes, such as DNA repair, genomic stability, and programmed cell death. At least 18 members of the PARP family are…
Tyrosine kinase is an enzyme that can transfer phosphate groups from ATP to tyrosine residues of specific proteins in cells. Specifically, this covalent post-translational modification is a key component of…
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…
Head and neck squamous cell carcinoma (HNSCC) represents more than 5% of all cancers each year. In addition, breast cancer is a heterogeneous group of diseases. Approximately 60-70% of breast…
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…
Repotrectinib is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. The IC50 values are 0.83/0.05/0.1 nM for TRKA/B/C, respectively. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib inhibits mutant ALKs. It inhibits…