Baricitinib is a small molecule inhibitor that is used for the treatment of rheumatoid arthritis. It was approved by the US Food and Drug Administration (FDA) in 2018. The drug is known to inhibit the activity of Janus kinase (JAK) enzymes, which are involved in the signaling pathways of cytokines and growth factors. This paper aims to provide a comprehensive review of baricitinib, including its method of synthesis, chemical structure, biological activity, applications, and future perspectives.
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EPZ005687 is a potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2). It acts competitively with the EZH2 substrate S-adenosylmethionine. EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against EZH1.1 It blocks trimethylation of the PRC2 target histone 3 lysine 27 (IC50 = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.1 A potent and selective small molecule inhibitor of histone methyltransferase EZH2 EPZ-005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases. IC50 Value: 24 nM (Ki)Target: EZH2in vitro: EPZ005687 shows concentration-dependent inhibition of PRC2 enzymatic activity with an IC50 value of 54 nM. It is a direct inhibitor of PRC2 enzymatic activity and does not function by disrupting the protein-protein interactions among the PRC2 subunits. EPZ005687 binds in the SAM pocket of the EZH2 SET domain and is a SAM-competitive inhibitor of EZH2 enzyme activity. The affinity of EPZ005687 is similar (within a two-fold range) for PRC2 complexes containing wild-type and Tyr641 mutant EZH2, but significantly greater affinity for the A677G mutant enzyme (5.4-fold). EPZ005687 reduces H3K27 methylation in various lymphoma cells. It shows robust cell killing in heterozygous Tyr641 or Ala677 mutant cells, with minimal effects on the proliferation of wild-type cells. EPZ005687 increases G1 phase of the cell cycle with correlative decreases in the S as well as the G2/M phases. In a Tyr641 mutant lymphoma cell line, EPZ005687 can lead to derepression of known EZH2 target genes and affect genes specifically repressed by the EZH2 Tyr641 mutant. in vivo:
Exenatide is a synthetic peptide that mimics the action of glucagon-like peptide-1 (GLP-1), a hormone that regulates glucose metabolism. It is used as a treatment for type 2 diabetes mellitus (T2DM) and obesity. Exenatide is a potent agonist of the GLP-1 receptor, which stimulates insulin secretion, suppresses glucagon secretion, and slows gastric emptying. This paper aims to provide a comprehensive review of exenatide, including its method of synthesis or extraction, chemical structure and biological activity, biological effects, applications, and future perspectives and challenges.
Cpda, also known as citrate-phosphate-dextrose-adenine, is a solution used for the preservation of red blood cells (RBCs) for transfusion purposes. It is a commonly used additive solution that helps to maintain the viability and functionality of RBCs during storage. Cpda is a complex solution that contains citrate, phosphate, dextrose, and adenine, which work together to provide the necessary nutrients and energy to RBCs.
Faropenem daloxate is a broad-spectrum antibiotic that belongs to the carbapenem class of antibiotics. It is used to treat a wide range of bacterial infections, including respiratory tract infections, urinary tract infections, skin and soft tissue infections, and intra-abdominal infections. Faropenem daloxate is a prodrug of faropenem, which is rapidly converted to the active form in the body.
DCPM is a synthetic compound that was first synthesized in 2005 by researchers at the University of California, San Francisco. Since then, it has been studied extensively for its potential therapeutic and environmental applications. DCPM is a pyrrole-based compound that contains two aromatic rings, one of which is substituted with two chlorine atoms and the other with a methoxy group. The compound also contains a morpholine ring and a pyrrole-2,5-dione ring. The unique chemical structure of DCPM makes it a promising candidate for various applications.
Tiletamine hydrochloride is a dissociative anesthetic drug that is commonly used in veterinary medicine. It is a potent anesthetic agent that is used in combination with other drugs to induce anesthesia in animals. Tiletamine hydrochloride is a Schedule III controlled substance in the United States and is only available for use by licensed veterinarians.
Miriplatin is a platinum-based anticancer drug that has been developed for the treatment of various types of cancer. It is a third-generation platinum complex that has shown promising results in preclinical and clinical studies.