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Supplementary information. Discovery of Novel STAT3 DNA Binding Domain Inhibitors

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posted on 28.06.2021, 09:59 authored by Adegboyega K. Oyelere, Bocheng Wu, Benny Payero, Sydney Taylor
Table S1

Description of synthesis

Spectra of synthesized compounds

Figure S1. Western blot gel for Compound 11c and 11d. MDA-MB-231 cell line treated by DMSO (0.1%), PYM 100µM, 11c (5 µM and 10 µM), 11d (5 µM and 10 µM) for 24 h. (a) gel of Actin, Bcl-2, and Bcl-xL. (b) Gel of Cyclin D1. (c) Gel for p-STAT3 and Actin. (d) Gel of T-STAT3 and Actin.

Figure S2. Western blot gel for Compound 11b and 15a. MDA-MB-231 cell line treated by DMSO (0.1%), PYM 100µM, 11b (5 µM and 10 µM), 15a (5 µM and 10 µM) in two separate experiments for 24 h. (a). gel of p-STAT3, GAPDH, Cyclin D1, Bcl-2, and Bcl-xL. (b). Gel of T-STAT3 and Actin.

Figure S3. Absorbance of NADPH without DHFR reduction.

Figure S4. Novel STAT3 inhibitor candidates do not inhibit DHFR activities. DHFR activity assay was performed with 1% provided hDHFR incubating with NADPH and DHFR substrate as the positive control. The treatment group was treated with 1% DMSO, or DMSO solution of PYM 500µM (2x IC50), 125 µM, 31.25 µM, 11b-d (10x IC50) and 15a (1x IC50) along with provided hDHFR, NADPH and DHFR substrate. DHFR activity was read at OD 340nm for NADPH absorbance with kinetic scanning (2-minute intervals from 0 to 28 minutes). The experiment was performed in duplicate data

Funding

Vasser-Woolley Fellowship

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