PKI-166 is a Selective and Orally Bioavailable EGFR Autophosphorylation Inhibitor
Human pancreatic cancer cells can secrete the proangiogenic molecules, such as VEGF, IL-8, and basic fibroblast growth factor. VEGF is the major proangiogenic factor in most types of human cancer. Therefore, in this article, we will introduce a potent, selective and orally active EGFR tyrosine kinase inhibitor, PKI-166. Firstly,...
BCI-215 is a Tumor Cell-Selective DUSP-MKP Inhibitor
Mitogen-activated protein kinase phosphatases (MKPs) belongs to the dual-specificity phosphatase (DUSP) family. DUSP-MKPs dephosphorylate and inactivate the MAPKs extracellular signal-regulated kinase (ERK), JNK/SAPK, and p38 on tyrosine and threonine residues. As a result, they result in regulating the duration and amplitude of mitogenic and survival signaling. There exists a ...
PF-573228 is a Potent and Selective FAK Inhibitor
Focal adhesion kinase (FAK) is a member of a family of non-receptor protein-tyrosine kinases. The FAK4 family kinases (which include FAK and Pyk2) regulate integrin and growth factor signaling pathways involved in cell migration, proliferation, survival. Besides, FAK expression is increased in many cancers, including breast and prostate cancer....
A-366 is a Potent Histone Methyltransferase G9a Inhibitor
Epigenetic alterations to the genome take place via modifications to the DNA or histones. Meanwhile, those modifications lead to changes in gene expression. Generally, histone lysine methylation is a prominent kind of epigenetic regulation for change of the structure chromatin and gene expression. HMTs have recently generated increasing interest...
AZD4547 is a Potent FGFR Family Inhibitor
Fibroblast growth factors (FGF) and their receptors play important roles in multiple biologic processes, such as tissue repair, hematopoiesis, angiogenesis, and embryonic development. The FGFR family mainly comprises 4 main members (FGFR1–4). FGFRs and FGFRs FGF ligand binding can result in FGFR dimerization. In addition, receptor autophosphorylation and activation...
CGP52411 is an Orally Active and ATP-Competitive EGFR Inhibitor
The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein that mediates the response of cells to EGF and transforming growth factor α. Deregulated signal transduction via the EGFR family of protein-tyrosine kinase growth factor receptors is relevant to proliferative diseases. Besides, the EGFR is involved in epithelial proliferation...
PI-103 is a Potent PI3K and mTOR Inhibitor
The phosphatidylinositide 3-kinase family possesses 15 members. those members consist of four distinct classes as a basis on their structure and biological properties. As we all know, this highly conserved family of enzymes involves various aspects of cellular homeostasis and exists a decline in a number of pathophysiologic conditions....