Tag: ERK

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...

CPL304110 is an Orally Active and Selective FGFR(1-3) Inhibitor

Over the last decade, the FGFRs family has become an attractive validated therapeutic target notably in cancer. It consists of four members (FGFR1 to FGFR4) which are structurally related cell surface RTKs. This FGF-FGFR axis participates in key biological processes that play significant roles in cell functions such as...