Category: 287192-97-6

Electric Literature of 287192-97-6, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.287192-97-6, Name is tert-Butyl 4-ethynylpiperidine-1-carboxylate, molecular formula is C12H19NO2. In a Article£¬once mentioned of 287192-97-6

Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands

Androgen receptor (AR) is a validated therapeutic target for the treatment of metastatic castration-resistant prostate cancer (mCRPC). We report herein our design, synthesis, and biological characterization of highly potent small-molecule proteolysis targeting chimera (PROTAC) AR degraders using a potent AR antagonist and E3 ligase ligands with weak binding affinities to VHL protein. Our study resulted in the discovery of 11 (ARD-266), which effectively induces degradation of AR protein in AR-positive (AR+) LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM. ARD-266 is capable of reducing the AR protein level by >95% in these AR+ prostate cancer cell lines and effectively reduces AR-regulated gene expression suppression. For the first time, we demonstrated that an E3 ligand with micromolar binding affinity to its E3 ligase complex can be successfully employed for the design of highly potent and efficient PROTAC degraders and this finding may have a significant implication for the field of PROTAC research.

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Piperidine – Wikipedia,
Piperidine | C5H15676N – PubChem

 

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬ name: tert-Butyl 4-ethynylpiperidine-1-carboxylate, Which mentioned a new discovery about 287192-97-6

SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT

Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as I useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 287192-97-6, help many people in the next few years.name: tert-Butyl 4-ethynylpiperidine-1-carboxylate

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Piperidine – Wikipedia,
Piperidine | C5H15642N – PubChem

 

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 287192-97-6, molcular formula is C12H19NO2, introducing its new discovery. , 287192-97-6

2,5-DIOXOIMIDAZOLIDIN-4-YL ACETAMIDES AND ANALOGUES AS INHIBITORS OF METALLOPROTEINASE MMP12

The invention provides compounds of formula (I) in which L, X, Y, Z1, Z2, R1, R2, R3 and G2 have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds of the invention are inhibitors of metalloproteinase MMP12 and are among other things useful for the treatment of obstructive airways diseases, such as asthma and chronic obstructive pulmonary disease (COPD).

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Piperidine – Wikipedia,
Piperidine | C5H15636N – PubChem