PIK-75 is a Reversible DNA-PK and p110α Selective Inhibitor
PI3Ks catalyze the phosphorylation of the D-3 position of the inositol headgroup of phosphatidylinositol leading to the synthesis of second messengers PtdIns3P, PtdIns(3,4)P2, PtdIns(3,5)P2 and PtdIns(3,4,5)P3. The p110α and p110β are the main forms in insulin target tissues. Especially, p110α isoform (PIK3CA) plays the predominant role in insulin signaling....
AGN194204 is an Orally Active and Selective RXR Agonist
Rexinoids are selective ligands for the retinoid X receptors (RXRα, RXRβ, and RXRγ). Specifically, rexinoids are multifunctional drugs that are useful for both the prevention and treatment of lung and breast cancer in preclinical animal models. Besides, retinoid X receptors heterodimerize with other receptors in the nuclear receptor superfamily. They modulate the activities of numerous steroid-like...
ADH-503 is an Orally Active and Allosteric CD11b Agonist
Integrin αMβ2 (CD11b/CD18) is a multifunctional integrin expressed on myeloid cells. In addition, CD11b/CD18 is an integrin molecule and plays an important role in their trafficking and cellular functions in inflamed tissues. Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal malignancy in which very limited responses to immunotherapy have been observed....
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,...
FPA-124 is a Selective Akt Inhibitor and Induces Apoptosis
Copper complexes play an important role in the active sites of a large number of metalloproteins in biological systems. Copper complexes also have a potential application for numerous catalytic processes in living organisms. In addition, copper complexes involve electron transfer reactions or activation of some antitumor substances. In this...
Niraparib is an Orally Active PARP Inhibitor
Poly (ADP-ribose) polymerases (PARPs) are a family of related enzymes. PARP shares the ability to catalyze the transfer of ADP-ribose to target proteins. PARP plays an important role in various cellular processes, including modulation of chromatin structure, transcription, replication, recombination, and DNA repair. Niraparib (MK-4827) is a potent PARP...
CCG-222740 is a Selective Rho/MRTF Pathway Inhibitor
Pancreatic cancer is one of the most lethal cancers, is characterized by a strong fibro-inflammatory reaction composed mainly of cancer-associated fibroblasts. Pancreatic stellate cells (PSCs) present in the pancreas tumor microenvironment. PSCs can excrete essential amino acids and cytokines to maintain an immunosuppressive environment. CCG-222740 is a potent and...