Tag: Anti-tumor

GN25 is a Specific p53-Snail Binding Inhibitor with Antitumor Effects

P53, also known as Tumor protein P53, or transformation-related protein 53 (TRP53) is a regulatory protein that is often mutated in human cancers. Besides, p53 is the strongest tumor suppressor gene. In addition, p53 also induces cell death, and growth arrest and suppresses metastasis in response to various kinds...

LY3177833 is an Orally Active CDC7 and pMCM2 Inhibitor

CDC7 is a serine/threonine kinase and plays an important role in the initiation of DNA replication. . In this article, we will introduce a potent CDC7 and pMCM2 inhibitor LY3177833. LY3177833 has an  IC50 of 3.3 nM against CDC7. Upregulation of CDC7 has been observed in numerous tumor cell...

CP681301 is a Potent CDK5 Inhibitor

CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. CDK5 is one of the Cyclin-dependent kinases. Importantly, CDK5 is an unconventional Cdk that regulates developmental and adult...

BM-1074 is a Potent and Specific Bcl-2/Bcl-xL Inhibitor

Bcl-2 (B-cell lymphoma 2) and Bcl-xL (B-cell lymphoma-extra large) are members of the Bcl-2 family of proteins. BCL-2 is localized to the outer membrane of mitochondria, where it plays an important role in promoting cell survival and inhibiting the actions of pro-apoptotic proteins. As well as, Bcl-xL acts as an...

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...