Alda-1 is a potent ALDH2 Agonist
Aldehyde dehydrogenase 2 (ALDH2) is ubiquitously found in various tissues, including the heart, brain, and skeletal muscle, and highly expressed in the mitochondria. Many cellular functions show relations with ALDH2. They include detoxification of aldehydes, cell survival, cell proliferation, and apoptosis. The deficiency of ALDH2 causes the accumulation of...
ABT-737 is a Selective and BH3 Mimetic Bcl-2, Bcl-xL and Bcl-w Inhibitor
Bcl-2 protein family is a key regulator of apoptosis and a marker of B-cell lymphoma. Importantly, apoptosis is an important physiological process of selective cell clearance, involving a variety of biological events. Particularly, the Bcl-2 family is the most characteristic protein family involved in regulating apoptotic cell death. It...
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...
Apitolisib is an Orally Active Class I PI3K and mTORC1/2 Inhibitor
Activation of the pathway occurs following activating point mutations or amplification of the PIK3CA gene encoding the p110a PI3K isoform. Oncogenes such as PI3K, AKT, epidermal growth factor receptor (EGFR), and human epithelial growth factor receptor 2 (HER2) stimulate proliferation, growth, and survival by activating mTOR kinase. The mTOR...
MS4322 is a First-in-Class PRMT5 PROTAC Degrader
PRMT5 is a member of type II protein arginine methyltransferases (PRMTs). When interacting with its binding partner MEP50, PRMT5 catalyzes monomethylation and symmetric dimethylation of arginine residues of its histone substrates. These substrates include H3R2, H3R8, and H4R3, and its nonhistone substrates, including p53, EGFR, N-MYC, SmD3, and RNA...
Zebularine is a DNA Methyltransferase Inhibitor
DNA methyltransferase (DNMT) family enzymes catalyze the transfer of methyl to DNA. Specifically, DNMT is a conserved cytosine methylase family, which plays a key role in epigenetic regulation. The DNMT family has four members, including DNMT1, Dnmt3a, DNMT3b, and DNMT3l. Different from other DNMTs, DNMT3l does not have any...
MRTX1133 is a Highly Selective, First-in-Class Inhibitor of KRAS G12D
Mutant KRAS is an attractive drug target for the treatment of a number of cancers for many decades. Until recently, the high affinity of KRAS for GDP/GTP and the lack of any other apparent binding pocket have significantly hampered the development of KRAS inhibitors. KRAS inhibitor relies on a...