SHR2415 is a Selective and Orally Active ERK1/2 Inhibitor
ERKs (extracellular signal-regulated kinases) are the original members of the mitogen-activated protein kinase (MAPK) family. They take part in the regulation of meiosis, mitosis, and postmitotic functions, thus, also influencing the development of cancer. ERK1 and ERK2 are important downstream points of the RAS-RAF-MEK-ERK signaling pathway. The two targets...
Ulixertinib is an Orally Active and ATP-Competitive ERK1/2 Inhibitor
Effective treatment for pancreatic ductal adenocarcinoma (PDAC) is an urgent, unmet medical need. Targeting KRAS, the oncogene that is present in >95% of PDAC, is a heavily pursued strategy but remains unsuccessful in the clinic. RAF or MEK inhibitors have failed to show clinical efficacy in PDAC. A report...
Chelerythrine is a Potent Protein kinase C Inhibitor
Chelerythrine is a natural benzo[c]phenanthridine alkaloid. It extracts from a number of plant species, such as Chelidonium majus, Macleaya cordata, Sanguinaria canadensis, etc. This compound exerts a wide spectrum of biological activities, including anti-cancer, anti-diabetes, anti-fungus, as well as a protective effect against the ethanol-induced gastric ulcer and the...
SHP394 is an Orally Active and Selective Inhibitor of SHP2
SH2 containing protein tyrosine phosphatase-2 (SHP2) is an oncogenic phosphatase. SHP2 facilitates growth and survival signaling downstream of numerous receptor inputs. In addition, higher levels of SHP2 phosphorylation associate with decreased survival of breast cancer patients. Especially, SHP394 is an orally active and selective inhibitor of SHP2. Pharmacological inhibition...
Rineterkib is an Orally Active RAF and ERK1/2 Inhibitor
ERK1 and ERK2 are related protein-serine/threonine kinases that participate in the Ras-Raf-MEK-ERK signal transduction cascade. This cascade participates in the regulation of a large variety of processes. It includes cell adhesion, cell cycle progression, cell migration, cell survival, differentiation, metabolism, proliferation, and transcription. MEK1/2 catalyze the phosphorylation of human...
IACS-13909 is a Selective and Orally Active SHP2 Inhibitor
Src homology 2 domain-containing phosphatase (SHP2) is a phosphatase that mediates signaling downstream of multiple receptor tyrosine kinases. SHP2 suppresses signaling through the MAPK pathway. Furthermore, SHP2 inhibition has demonstrated tumor growth inhibition in receptor tyrosine kinases-activated cancers. In this study, researchers report the discovery of IACS-13909. IACS-13909 is...
ML786 is an Orally Bioavailable Raf Inhibitor
The mitogen-activated protein kinase (MAPK) signal pathway plays an important role in cells. It also has a response to many different external stimuli and regulates cellular growth, proliferation. The Raf isoform B-Raf is one component of this pathway. Besides, it has a high rate of activating mutation in melanoma...