Johnson, Ronald L. published the artcileA quantitative high-throughput screen for modulators of IL-6 signaling: A model for interrogating biological networks using chemical libraries, Synthetic Route of 330161-87-0, the publication is Molecular BioSystems (2009), 5(9), 1039-1050, database is CAplus and MEDLINE.
Small mol. modulators are critical for dissecting and understanding signaling pathways at the mol. level. Interleukin 6 (IL-6) is a cytokine that signals via the JAK-STAT pathway and is implicated in cancer and inflammation. To identify modulators of this pathway, we screened a chem. collection against an IL-6 responsive cell line stably expressing a β-lactamase reporter gene fused to a sis-inducible element (SIE-bla cells). This assay was optimized for a 1536-well microplate format and screened against 11 693 small mols. using quant. high-throughput screening (qHTS), a method that assays a chem. library at multiple concentrations to generate titration-response profiles for each compound The qHTS recovered 564 actives with well-fit curves that clustered into 32 distinct chem. series of 13 activators and 19 inhibitors. A retrospective anal. of the qHTS data indicated that single concentration data at 1.5 and 7.7 μM scored 35 and 71% of qHTS actives, resp., as inactive and were therefore false negatives. Following counter screens to identify fluorescent and non-selective series, we found four activator and one inhibitor series that modulated SIE-bla cells but did not show similar activity in reporter gene assays induced by EGF and hypoxia. Small mols. within these series will make useful tool compounds to investigate IL-6 signaling mediated by JAK-STAT activation.
Molecular BioSystems published new progress about 330161-87-0. 330161-87-0 belongs to indole-building-block, auxiliary class Protein Tyrosine Kinase/RTK,Src, name is SU6656, and the molecular formula is C19H21N3O3S, Synthetic Route of 330161-87-0.
Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles