DGY-06-116 is an Irreversible Covalent and Selective Src Inhibitor
Src kinase family is a family of non-receptor tyrosine kinases. DGY-06-116 is a selective Src inhibitor. DGY-06-116 is an SRC-directed covalent kinase inhibitor that displays efficient covalent target labeling and irreversible cellular inhibition of SRC signaling. Furthermore, DGY-06-116 inhibits SRC for an extended duration, likely due to its ability...
DT-061 is an Orally Active PP2A Activator
Protein phosphatase 2A (PP2A) comprises a family of serine/threonine phosphatases, minimally containing a well-conserved catalytic subunit. PP2A plays a prominent role in the regulation of specific signal transduction cascades. Additionally, PP2A interacts with a substantial number of other cellular and viral proteins. DT-061 is an orally bioavailable small-molecule activator...
BDTX-189 is an Orally Active Inhibitor of Allosteric EGFR and HER2 Oncogenic Mutations
Epidermal growth factor receptor (EGFR) is a growth-factor-receptor tyrosine kinase. Elevated levels of the EGFR, and/or its cognate ligands act as a common component of multiple cancer types and appear to promote solid tumor growth. BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations....
CMLD-2 is Inhibits HuR and Induces Apoptosis
Hu antigen R (HuR) is an RNA binding protein. Specifically, Its overexpression in human cancer is associated with aggressive disease, drug resistance, and poor prognosis. HuR is highly abundant in many types of cancer and promotes tumorigenesis through cancer-related mRNA interactions. Besides, HuR has related to the regulation of...
Afatinib is an Irreversible and Orally Active EGFR Family Inhibitor
Lung cancer continues to be the leading cause of cancer-related mortality. Members of the ERBB receptor tyrosine kinase family include EGFR, HER2, HER3, and HER4. They present an attractive option for targeted therapy in patients with NSCLC, due to observed patterns of oncogenic mutation of EGFR and HER2. In addition, esophageal...
CTPI-2 is a Mitochondrial Citrate Carrier SLC25A1 Inhibitor
Nonalcoholic fatty liver disease (NAFLD) and inflammatory steatohepatitis (NASH) comprise a series of manifestations that span from reversible hepatic steatosis to progressive necroinflammatory and fibrotic disease. There exists a clear association between NASH with obesity, diabetes, and metabolic syndrome. Slc25a1 is a mitochondrial citrate carrier, which belongs to a...
EMI56 is a Superior Mutant EGFR Inhibitor
Receptor Tyrosine Kinases (RTKs) play critical roles in embryogenesis, normal physiology, and several diseases. Epidermal growth factor receptor (EGFR) is a transmembrane protein with cytoplasmic kinase activity that transduces important growth factor signaling from the extracellular milieu to the cell. Furthermore, EGFR common double mutations include 19Del, L858R, and...