J9集团

The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/β-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer. SAR analysis leads to the identification of a number of potent TNIK inhibitors with Compound 21k being the most active one. Preliminary assessment for the pharmacokinetic properties of 21k was carried out through services provided by Medicilon.

Nonalcoholic steatohepatitis (NASH) is the advanced subtype of nonalcoholic fatty liver disease (NAFLD) and is becoming a severe global public health problem. PPARα/δ are regarded as potential therapeutic targets for NASH. Herein, researchers report a series of novel triazolone derivatives as PPARα/δ dual agonists. The pharmacokinetic studies were conducted by Medicilon. The hERG channel inhibition studies were conducted by Medicilon. The Ames tests were conducted by Medicilon.

A PROTAC-based androgen receptor (AR) degrader is a bifunctional small molecule, consisting of an AR ligand that binds to AR protein, and a ligand that binds to and recruits an E3 ligase complex, tethered together through a linker. Researchers report the discovery of exceptionally potent and orally bioavailable PROTAC AR degrader ARD-2585 (Compound 43). ARD-2585 is a promising AR degrader for extensive investigations for the treatment of advanced prostate cancer. The liver microsomal stability assay was performed by Medicilon. The plasma stability assay was performed by Medicilon. The hERG assay was performed by Medicilon.

Cancer is one of the leading causes of death worldwide. MYC oncogene is involved in the majority of human cancers and is often associated with poor outcomes. WBC100, a novel oral active molecule glue that selectively degrades c-Myc protein over other proteins and potently kills c-Myc overexpressing cancer cells is reported. Researchers performed direct binding assay of WBC100 with c-Myc on biosensor chip by surface plasmon resonance (SPR). SPR experiments were performed using a Biacore T200 instrument by Medicilon.

SAHA was synthesized by Medicilon and was given to mice as 50?mg/kg doses. Injections (10?mL/kg) were given intraperitoneally and were alternated daily between left and right sides of the abdomen. Chronic treatments of SAHA completely restored performance deficits in APP/PS1 mice.

TAK-243 is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE), the primary mammalian E1 enzyme that regulates the ubiquitin conjugation cascade. TAK-243 has UAE-specific antitumor efficacy in vivo. Medicilon performed the experiment using the HCC70 (triple-negative breast cancer) model.

Pharmacokinetic studies revealed that after a single oral dose, the FTI (LNK-754) was cleared from plasma within 20 hours and could rapidly cross the blood-brain-barrier. Pharmacokinetic analysis was performed as a service provided by Medicilon.

The binding assay by surface plasmon resonance (SPR) analysis shows that WYC-209A and WYC-209B acid bind to RARs at nano-molar doses. SPR was carried out by Medicilon, using the Biacore 8K equipment.

ARD-2128 has excellent plasma and microsomal stability in all the five species (Human, Mouse, Rat, Dog, and Monkey). The in vitro stability and pharmacokinetic (PK) studies were performed by Medicilon.

Human dihydroorotate dehydrogenase (DHODH) is a viable target for the development of therapeutics to treat cancer and immunological diseases. Herein, researchers designed and synthesized a series of acrylamide-based novel DHODH inhibitors as potential rheumatoid arthritis (RA) treatment agents.