Month: January 2021

Afatinib is an Irreversible and Orally Active EGFR Family Inhibitor

Lung cancer continues to be the leading cause of cancer-related mortality. Members of the ERBB receptor tyrosine kinase family include EGFR, HER2, HER3, and HER4. They present an attractive option for targeted therapy in patients with NSCLC, due to observed patterns of oncogenic mutation of EGFR and HER2. In addition, esophageal...

NSC-105808 is a Specific DNA2 Nuclease Inhibitor with Antitumor Activity

DNA2 nuclease possesses 5′ flap endonuclease and 3′-5′ helicase activities. It has an important role in DNA damage repair, homologous recombination, and DNA replication. The nuclease activity of DNA2 has several well-documented cellular functions. However, the biological role of its helicase activity remains enigmatic. DNA2 mediates the resection of...

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...

R59949 is a pan Diacylglycerol Kinase (DGK) Inhibitor

Diacylglycerol kinase (DGK) is a second messenger in its own right and can modulate the activity of PKC and several ion channels.  Chemokines are low MW extracellular signaling peptides secreted by tissue either constitutively during homeostasis or de novo during an inflammatory response. They are a diverse family of...

G5-7, an Orally Active JAK2 Inhibitor, Induces Cell Cycle Arrest and Apoptosis

JAK2 and STAT3 have been extensively implicated in the development and progression of numerous cancers. STAT3 be also activated by EGFR, JAK2, and other TYKs activated by EGF, LIF, and other cytokines. STAT3 constitutively activats in 60% of primary malignant gliomas, and the extent of activation correlates with glioma...

NSC 80467 is a DNA Damaging Agent and a Selective Survivin Suppressant

Each of the ~1013 cells in the human body receives tens of thousands of DNA lesions per day. These lesions can block genome replication and transcription. If they are not repaired or are repaired incorrectly, they lead to mutations or wider-scale genome aberrations that threaten cell or organism viability....

CJ-2360 is a Potent and Orally Active ALK Inhibitor

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase belonging to the insulin receptor (IR) kinase superfamily. It highly expresses in adult brain tissue and exerts an important role in the development of the nervous system. Deregulation of ALK originally presents by the identification of at (2;5) chromosomal translocation...