WebThe inhibitory activity of putative kinase inhibitors and the potency of selected compounds are determined using a trans-phosphorylation assay. Specific peptide or protein … WebStep 1: Make a 100-nM peptide stock in CRB (use the same peptide substrate as in the kinase assay). Step 2: Make a 100-nM phosphopeptide stock in CRB (use the phosphorylated version of the substrate used in the kinase assay). Step 3: Combine peptide and phosphopeptide stocks to make calibration standards as indicated in Table 1.
Establishing and optimizing a fluorescence polarization assay
Web1 de dez. de 2024 · Onvansertib (also known as PCM-075 or NMS-1286937) is a selective ATP-competitive PLK1 inhibitor. Biochemical assays demonstrated high specificity of … Web5 de jul. de 2024 · a) Global analysis of FP curves from the direct titration of probe (10 nM) with midkine (12 – 750 nM) and from a competitive assay consisting of a sample with probe (10 nM) and midkine (63 nM) where … nbc the olympics
Fluorescence Polarization Assays for Drug Discovery
Web1 de dez. de 2009 · When developing an FP assay to target a protein-peptide or protein–nucleic acid interaction, a number of key strategic considerations are involved in … WebBI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. ... Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, ... Web29 de abr. de 2016 · Figure 1. The basic principle of fluorescence polarization. A fluorescent probe is excited with polarized light (I ǁ) and emits after the fluorescence lifetime (τ) of the probe.Emission intensity is measured in orientations that are parallel (I ǁ) and perpendicular (I ┴) to the excitation plane.The extent to which the emitted fluorescence remains … nbc there\u0027s something about pam