Sotorasib (AMG-510) is an Orally Bioavailable KRAS G12C Covalent Inhibitor
The KRAS oncoprotein is a GTPase and an essential mediator of intracellular signaling pathways. KRAS oncoprotein regulates tumor cell growth and survival. However, KRAS also is the most frequently mutated oncogene in cancer and encodes a key signaling protein in tumors. In addition, KRASG12C mutant is present in approximately...
SU056, a YB-1 Inhibitor, Induces Cell-cycle Arrest, Apoptosis and Inhibits Cell Migration in Cancer
Y-box-binding proteins (YB proteins) belong to a family of proteins that contain a cold shock domain. The YB protein consists of three members, YB-1, YB-2 and YB-3. Among the YB proteins, YB-1 is the most widely studied one, which plays important roles in DNA repair, cell proliferation and differentiation....
SH-BC-893 is an Orally Active Anti-neoplastic Sphingolipid Analog
Cancer and metabolism-related diseases have a significant impact on humans. Cancer cells are constitutively anabolic. It will cause quiescence and catabolism in normal cells because of they are unable to tolerate nutrient stress. So, oncogenic mutations will reselect the metabolic circuitry during the tumorigenic process to meet the increased...
ARN24139 is a TopoII Inhibitor with Promising Antiproliferative Activity
Topoisomerase II is a ubiquitous enzyme in all branches of life that alters DNA supercoils and breaks double-stranded DNA fragments during processes such as replication and transcription. Eukaryotic Topoisomerase II functions as a homodimer and requires ATP and divalent metal ions for overall catalytic activity. It interconverts different topologies...
YX-2-107, a PROTAC, is a Selective CDK6 Degrader
Ph+ALL (Philadelphia chromosome-positive acute lymphoblastic leukemia) is a rare subtype of leukemia characterized by the abnormal formation of the Philadelphia chromosome, which occurs when pieces of chromosomes 9 and 22 switch with each other. The incidence of Ph+ ALL increases with age, and occurs in up to 50 %...
D6808 is a Highly Selective c‑Met Inhibitor used for NSCLC and Gastric Cancer Research
c-Met is a unique subfamily member of receptor tyrosine kinase (RTK) behaving as the receptor of hepatocyte growth factor (HGF)/scatter factor (SF). The HGF/c-Met signaling pathway plays important roles in a variety of biological activities. However, aberrant HGF/c-Met signaling is associated with the induction of a multitude of human...
Manzamine A, an Orally Active β-Carboline Alkaloid with Antiviru, Antimalarial and Anticancer Activities
AManzamine A is an orally active β-carboline alkaloid effective against HSV-1, Cancer, and Malaria. For HSV-1， It is estimated that approximately 80% of the population worldwide are carriers of HSV-1 and approximately 40% suffer from recurrent infections. Unfortunately, this recurrent nature is a leading cause of corneal disease and...