| Solution Information | help | |
| Enzyme: | Induced myeloid leukemia cell differentiation protein Mcl-1 | |
| inhibitor: | BDBM50675 | |
| substrate: | n/a | |
| Solution Type: | Aqueous | |
| pH at Preparation: | n/a | |
| Temp. Prep.: | n/a | |
| Comments: | Assay Overview: The purpose of this assay is to determine dose response curves for compounds identified as active in a set of previous experiments entitled, "Fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of myeloid cell leukemia sequence 1 (MCL1) interactions with BIM-BH3 peptide" (AID 2057), and that confirmed activity in a set of experiments entitled, "Fluorescence polarization-based biochemical high throughput confirmation assay for inhibitors of myeloid cell leukemia sequence 1 (MCL1) interactions with BIM-BH3 peptide (AID 2168). This biochemical assay monitors binding of the BH3 domain of the Bcl-2 family member, Bim, to the binding pocket of human MCL1. In this fluorescence polarization (FP)-based assay, GST-MCL1 fusion protein is incubated with FITC-BH3-Bim peptides, in the presence of test compounds. Binding of peptide to MCL1 target protein increases the effective molecular mass of the peptide, slowing its rotation | |
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