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...
MC2590, a Potent HDAC Inhibitor, inhibits HDAC1-3, -6, -8, and -10
Histone deacetylase (HDAC) is an epigenetic enzyme that regulates gene expression through histone deacetylation. It leads to more closed chromatin structure and gene expression inhibition. Many non-histones are also targets of HDAC, such as α Microtubulin, heat shock protein (HSP) 90, and hypoxia-inducible factor HIF-1 α. Specifically, HDAC is...
LCS3 is a Glutathione Disulfide Reductase (GSR) and TXNRD1 Inhibitor
Glutathione Disulfide Reductase (GSR), also known as glutathione reductase (GR), catalyzes the reduction of glutathione disulfide (GSSG) to glutathione (GSH) in the presence of NADPH and flavin adenine dinucleotide (FAD). GSH acts as a scavenger of reactive oxygen species (ROS) such as free radicals, peroxides, lipid peroxides and heavy...
Almonertinib is an Orally Active and Irreversible EGFR Inhibitor
Lung cancer is one of the most common malignant tumors in the world. Its lethality ranks the first among many malignant tumors. In addition, the overexpression of the human ATP-binding cassette (ABC) drug transporter ABCB1 (P-gp) or ABCG2 (BCRP) in cancer cells often contributes significantly to the development of...
DT-061 is an Orally Active PP2A Activator
Protein phosphatase 2A (PP2A) comprises a family of serine/threonine phosphatases, minimally containing a well-conserved catalytic subunit. PP2A plays a prominent role in the regulation of specific signal transduction cascades. Additionally, PP2A interacts with a substantial number of other cellular and viral proteins. DT-061 is an orally bioavailable small-molecule activator...
Cilengitide is a Selective Integrin Inhibitor for αvβ3 and αvβ5 Receptor
Integrins are heterodimeric cell surface adhesion receptors that consist of two noncovalently associated alpha and beta subunits. In particular, Integrins are heterodimeric transmembrane proteins composed of one α and one β subunit. Especially, Integrins are crucially important because they are the main receptor proteins that cells use to bind...
BM-1197 is a Potent and Selective Dual Bcl-2/Bcl-xL Inhibitor
Bcl-2 and Bcl-xL are critical regulators of apoptosis. The pharmacological inhibition of Bcl-2 and Bcl-xL represents a promising strategy for cancer treatment. In addition, BM-1197 is a potent and efficacious dual inhibitor of Bcl-2 and Bcl-xL. BM-1197 binds to Bcl-2 and Bcl-xL proteins with Ki values less than 1...