a reversible and highly selective inhibitor of

a reversible and highly selective inhibitor of

  • a reversible and highly selective inhibitor of the proteasomal ubiquitin receptor rpn13 is toxic to multiple myeloma cells

    A Reversible and Highly Selective Inhibitor of the Proteasomal Ubiquitin Receptor Rpn13 Is Toxic To Multiple Myeloma Cells

    20/5/2015 · Here we describe the discovery of the first highly selective, reversible Rpn13 ligands and show that they are also selectively toxic to MM cells. These data strongly support the hypothesis that Rpn13 is a viable target for the development of

  • a reversible and highly selective inhibitor of the proteasomal ubiquitin receptor rpn13 is toxic to multiple myeloma cells | journal of the

    A Reversible and Highly Selective Inhibitor of the Proteasomal Ubiquitin Receptor Rpn13 Is Toxic to Multiple Myeloma Cells | Journal of the

    Here we describe the discovery of the first highly selective, reversible Rpn13 ligands and show that they are also selectively toxic to MM cells. These data strongly support the hypothesis that Rpn13 is a viable target for the development of

  • ag 1478 - cas 175178-82-2 - calbiochem a cell-permeable, reversible, atp-competitive, highly potent and selective inhibitor of epidermal growth

    AG 1478 - CAS 175178-82-2 - Calbiochem A cell-permeable, reversible, ATP-competitive, highly potent and selective inhibitor of epidermal growth

    General description A cell-permeable, reversible, ATP-competitive, highly potent and selective inhibitor of epidermal growth factor receptor kinase (IC 50 = 3 nM) versus HER2-neu (IC 50 >100 µM) and platelet-derived growth factor receptor

  • evaluation of jak3 biology in autoimmune disease using a highly selective, irreversible jak3 inhibitor - pubmed

    Evaluation of JAK3 Biology in Autoimmune Disease Using a Highly Selective, Irreversible JAK3 Inhibitor - PubMed

    Reversible JAK3 inhibitors cannot achieve sufficient selectivity against other isozymes in the cellular context due to inherent differences in enzyme ATP K m values. Therefore, we developed irreversible JAK3 compounds that are potent and highly

  • development of a selective aldh2 inhibitor to treat aud - full text view - clinicaltrials.gov

    Development of a Selective ALDH2 Inhibitor to Treat AUD - Full Text View - ClinicalTrials.gov

    Unlike disulfiram, a non-selective and irreversible ALDH2 and ALDH1 inhibitor, which produces an aversive flushing response, the oral ANS-6637 compound is a selective and reversible inhibitor of ALDH2 that attenuates the surge in dopamine (DA).

  • preclinical and early clinical profile of a highly selective and potent oral inhibitor of aldosterone synthase (cyp11b2) - pubmed

    Preclinical and Early Clinical Profile of a Highly Selective and Potent Oral Inhibitor of Aldosterone Synthase (CYP11B2) - PubMed

    Preclinical and Early Clinical Profile of a Highly Selective and Potent Oral Inhibitor of Aldosterone Synthase (CYP11B2) Hypertension. 2017 Jan;69(1):189-196. doi: 10.1161/HYPERTENSIONAHA.116.07716. Epub 2016 Nov 21

  • aurora a inhibitor | aurora a selective inhibitors | aurora a isoform specific inhibitor

    Aurora A inhibitor | Aurora A Selective inhibitors | Aurora A isoform specific inhibitor

    Catalog No. Product Name Information Selective / Pan IC50 / Ki S2770 MK-5108 (VX-689) MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it

  • discovery and characterization of a highly selective faah inhibitor that reduces inflammatory pain: chemistry & biology

    Discovery and Characterization of a Highly Selective FAAH Inhibitor that Reduces Inflammatory Pain: Chemistry & Biology

    Here, we report the discovery and detailed characterization of a highly efficacious and selective FAAH inhibitor, PF-3845. Mechanistic and structural studies confirm that PF-3845 is a covalent inhibitor that carbamylates FAAH's serine

  • discovery and characterization of highly potent and selective allosteric usp7 inhibitors | nature chemical biology

    Discovery and characterization of highly potent and selective allosteric USP7 inhibitors | Nature Chemical Biology

    4/12/2017 · A selective inhibitor of the deubiquitinase USP7 binds an allosteric site to inhibit its MDM2-stabilizing activity, resulting in stabilization of p53 and p21, which confers hypersensitivity to

  • phase 1, first-in-human study of futibatinib, a highly selective, irreversible fgfr1–4 inhibitor in patients with advanced solid tumors

    Phase 1, First-in-Human Study of Futibatinib, a Highly Selective, Irreversible FGFR1–4 Inhibitor in Patients with Advanced Solid Tumors

    2/7/2020 · Background Futibatinib is an oral, irreversible, highly selective fibroblast growth factor receptor (FGFR)1–4 inhibitor with potent preclinical activity against tumors harboring FGFR aberrations. This first-in-human, phase 1 dose-escalation

  • discovery of a potent and highly selective pdk1 inhibitor via fragment-based drug discovery - sciencedirect

    Discovery of a potent and highly selective PDK1 inhibitor via fragment-based drug discovery - ScienceDirect

    15/5/2011 · Discovery of a potent and highly selective PDK1 inhibitor via fragment-based drug discovery Author links open overlay panel Daniel A. Erlanson a Joseph W. Arndt b Mark T. Cancilla a Kathy Cao a Robert A. Elling a Nicki English b Jessica Friedman