GNE-618 is a Orally Active NAMPT Inhibitor
Nicotinamide adenine dinucleotide (NAD) is a critical metabolite for a range of cellular reactions. NAD is an essential coenzyme involved in cellular redox reactions and is a substrate for NAD-dependent enzymes. Especially, Nicotinamide phosphoribosyltransferase (Nampt) is an enzyme necessary for NAD synthesis. Nampt catalyzes the rate-limiting step leading to...
S516 is a Potent Tubulin Polymerization Inhibitor
The microtubules act as an attractive target for anticancer drug discovery nowadays. Disruption of microtubules can induce cell cycle arrest in the G2-M phase and formation of abnormal mitotic spindles. The tubulin polymerization inhibitors have emerged as one of promising anticancer therapeutics because of their dual mechanism of action,...
AC-73 is a Specific and Orally Active CD147 Dimerization Inhibitor
Hepatocellular carcinoma (HCC) is one of the most common cancers. Combating hepatocellular carcinoma invasion and metastasis has become a major desire in hepatocellular carcinoma patients. CD147 (also called EMMPRIN) is a member of the immunoglobulin superfamily. AC-73 is the first specific inhibitor of CD147. In particular, CD147 is a...
DS18561882 is Selective and Orally Active MTHFD2 Inhibitor
The human mitochondrial enzyme, called methylenetetrahydrofolate dehydrogenase 2 (MTHFD2), plays a key role in one-carbon metabolism in purine or thymidine biosynthesis. In mitochondrial folate carbon metabolism, MTHFD2 has attracted considerable attention as a potential target for cancer treatment. Its inducement is a higher expression in various human tumor types,...
CP5V is a Specific PROTAC Degrader of Cdc20
The cell-division cycle protein 20 (Cdc20) is the substrate receptor of anaphase synthesis complex (APC) or cyclosome (APC/C). Besides, it coordinates late initiation and exit of mitosis through safety and time-dependent degradation. Cdc20 is a key mitotic factor, which controls the beginning of anaphase and the exit of mitosis....
AG-825, a selective ErbB2 inhibitor with anti-cancer effect
The ErbB tyrosine kinase receptor (RTK) family has 4 members: ErbB1 (EGFR/HER1), ErbB2 (HER2/neu), ErbB3 (HER3), and ErbB4 (HER4). These receptors are cell surface receptors and play important roles in cell proliferation, survival, and growth signaling. ErbB2 is an orphan receptor; it can associate with other ErbBs to enhances...
MRTX849 is an Orally Active and Covalent Inhibitor of KRAS G12C
KRAS mutations are the most common mutations. Especially, the KRAS oncogene encodes a binding protein that plays a crucial role in transmitting signals from extracellular growth factors to the cell nucleus. KRAS mutations occur commonly in colorectal carcinomas. KRASG12C mutations are present in lung and colon adenocarcinoma as well...