• We are sorry, but NCBI web applications do not support your browser and may not function properly. More information

Table of Assay Rationale and Screening Statistics

AIDAssay RationaleAssay DescriptionZ′S:B
862Identify compounds that inhibit STAT3.A human U3A fibrosarcoma cell line (deficient in STAT1) stably expressing a human STAT3-luciferase construct is incubated with test compounds and IL-6. Well luminescence is read after 6 hours.0.846.22
920Identify compounds that inhibit STAT1.A murine NIH 3T3 fibroblast cell line stably expressing STAT1-luciferase is incubated with test compounds and IFNγ. Well luminescence is read after 6 hours.0.8111.00
1265Confirm activity of compounds active in AID-862.Same as AID-862 except that compounds are tested in triplicate.0.888.04
1308Determine whether compounds active in AID-862 were nonselective due to inhibition of NFκB.A human HEK 293T cell line stably expressing a human NFκB::luciferase construct is incubated with test compounds in the presence of TNFα. Well luminescence is read after 6 hours. Compounds are tested in triplicate.0.8717.60
1317Determine whether compounds active in AID-862 were nonselective due to inhibition of STAT1.Same as AID-920 except that compounds are tested in triplicate.0.877.29
1399Determine STAT3 inhibition dose response curves for compounds active inAID-862.Same as AID-862 except that compounds are tested in triplicate using a 10-point dilution series starting at 55.7 μM.0.826.88
1411Determine STAT1 inhibition dose response curves for compounds active in AID-862.Same as AID-920 except that compounds are tested in triplicate using a 10-point dilution series starting at 55.7 μM.0.8614.58
1806Summarize probe development efforts.N/AN/AN/A
2078Describe the assays performed during the probe development effort.STAT3 Inhibition Assays, STAT1 Inhibition Counterscreen Assays, NFkB Inhibition Counterscreen Assay as above, plus additional assays to determine compound cytotoxicity.N/AN/A

From: Modulators of STAT Transcription Factors for the Targeted Therapy of Cancer (STAT3 Inhibitors)

Cover of Probe Reports from the NIH Molecular Libraries Program
Probe Reports from the NIH Molecular Libraries Program [Internet].

NCBI Bookshelf. A service of the National Library of Medicine, National Institutes of Health.