CAY10404 is a Highly Selective COX-2 Inhibitor
Clooxygenase (COX) is an enzyme responsible for the formation of prostaglandins from arachidonic acid, including thromboxanes and prostaglandins. Specifically, it is a member of the animal heme peroxidase family, also known as prostaglandin G/H synthase. Besides, cyclooxygenase-2 is a candidate gene for lung injury induced by mechanical ventilation. COX-2...
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...
MCP110 is an Inhibitor of Ras/Raf-1 Interaction
Ras is a small GTPase and interacts with the protein Raf to create activated Ras-Raf complex that activates the downstream effectors in the ERK pathway. Malfunctioning Ras-Raf switches cause cancer. Ras-Raf interaction has taken a center stage in cancer research. Ras is a peripheral membrane protein that acts as...
DM-01 is a Powerful and Selective EZH2 Inhibitor
Enhancer of zeste homolog 2 (EZH2) is a histone methyltransferase and a catalytic component of polycomb repressive complex 2 (PRC2). EZH2 catalyzes tri-methylation of histone H3 at Lys 27 (H3K27me3) to regulate gene expression through epigenetic machinery. In addition, EZH2 also functions both as a transcriptional suppressor and a...
JX06 is a Potent, Selective and Covalent Inhibitor of PDK
Pyruvate dehydrogenase kinase (PDK) is a kinase that can be inactivated by the use of ATP phosphorylation of pyruvate dehydrogenase. Specifically, PDK is relevant to the regulation of the pyruvate dehydrogenase complex with pyruvate dehydrogenase as the first component. Besides, PDK acts as a molecular switch to reduce mitochondrial...
RBN-2397 is a Selective and Orally Active NAD+ Competitive PARP7 Inhibitor
PARP is a family of proteins involved in a number of cellular processes involving mainly DNA repair and programmed cell death. The PARP family comprises 17 members. PARP1, PARP2 (inhibitor Olaparib), and PARP7 are all potential anti-cancer targets. PARP7 is a member belongs to the monoPARP family. The function...
ONO-7475 is a Selective and Orally Active AXL/Mer Inhibitor
EGFR tyrosine kinase inhibitors (EGFR-TKIs) are efficient for the treatment of non-small cell lung cancer (NSCLC) harboring EGFR mutations. However, most EGFR-positive NSCLC patients exhibit resistance to EGFR-TKIs after sometimes. The 3rd generation EGFR-TKI Osimertinib shows efficacy for overcoming EGFR T790M mutation-positive NSCLC. Anexelekto (AXL) belongs to the TAM...