Mirin is a Potent Mre11-Rad50-Nbs1 (MRN) Complex Inhibitor
ATM belongs to the phosphatidylinositol-3′ kinase-related kinase (PIKK) family. It has a critical role in the maintenance of genome integrity. In response to agents that generate DNA double-strand breaks (DSBs), inactive dimeric ATM protein dissociates into phosphorylated monomers. The MRN (Mre11-Rad50-Nbs1)-ATM pathway is essential for sensing and signaling from...
BM213 is a Potent and Selective Agonist of Complement C5a Receptor 1
The complement factor C5a is a 74-residue glycopolypeptide central to the complement system. “C5 convertase” cleaves the precursor C5 protein and it becomes the complement factor C5a. It mediates inflammation through the recruitment of leukocytes (such as neutrophils and macrophages), induction of cytokine release and neutrophil degranulation. C5a binds...
AUTAC2 is a FKBP12-Targeting Autophagy-Mediated Degrader (AUTAC)
Autophagy-targeting chimera (AUTAC) is a technology that selectively degrades intracellular proteins and intracellular debris through the autophagy pathway. An AUTAC molecule contains a degradation tag (guanine derivative) and a ligand of the protein of interest (POI) to provide target specificity. AUTAC can selectively recognize and degrades a broad range...
Linzagolix is a potent, non-Peptide, and Orally Active GnRH Antagonist
Uterine myomas and endometriosis are sex-hormone-dependent diseases. They affect up to 50-60% and 10-50% women of reproductive age, respectively. Endometriosis is an estrogen-dependent chronic inflammatory disease. The pathophysiology of this complex disease is multifactorial: in its pathogenesis, hormonal dysfunction, and proinflammatory microenvironment of eutopic and ectopic endometrium play a...
Tanomastat is an Orally Bioavailable, non-Peptidic Biphenyl MMPs Inhibitor
Matrix metalloproteinases (MMPs) are zinc-dependent endopeptidases. The MMPs belong to a larger family of proteases known as the metzincin superfamily. MMPs are capable of degrading all kinds of extracellular matrix proteins, but also can process a number of bioactive molecules. The activity of MMPs is thought to be balanced...
Chelerythrine is a Potent Protein kinase C Inhibitor
Chelerythrine is a natural benzo[c]phenanthridine alkaloid. It extracts from a number of plant species, such as Chelidonium majus, Macleaya cordata, Sanguinaria canadensis, etc. This compound exerts a wide spectrum of biological activities, including anti-cancer, anti-diabetes, anti-fungus, as well as a protective effect against the ethanol-induced gastric ulcer and the...
PX-12 is an Irreversible Inhibitor of Thioredoxin-1 (Trx-1)
Colorectal cancer is one of the leading causes of cancer-related mortality in most industrialized nations. It needs to find an effective adjuvant therapy for colorectal cancer. There includes non-steroidal anti-inflammatory drugs, immunotherapy, and gene therapy. Thioredoxin (Trx) and thioredoxin reductase 1 are among the major redox regulators in mammalian...