bet inhibitors  (MedChemExpress)

Journal: Non-coding RNA

Article Title: Bromodomain and Extra-Terminal Family Proteins BRD2, BRD3, and BRD4 Contribute to H19-Dependent Transcriptional Regulation of Cell Adhesion Molecules, Modulating Metastatic Dissemination Program in Prostate Cancer.

doi: 10.3390/ncrna11030033

Figure Lengend Snippet: Figure 3. Effect of several BET family protein inhibitors, BRD2/3/4 or BRD7/9 members, on the gene expression level of E-cadherin and β4 integrin and cell proliferation. E-cadherin (CDH1, (A)), β4 integrin (ITGB4, (B)), Cyclin D1 (CCND1, (C)), Vimentin (VIM, (D)), and c-Myc (E) mRNAs were assessed by qPCR in PC-3-luc (PC-3), 22Rv1-luc (22Rv1), and Du145 in presence or absence of 48 h treatment with BRD2/3/4 family inhibitors, JQ1, dBET6, OTX015 (OTX), or BRD7/9, inhibitor Bi7273, or inactive (R)-(-)-JQ1 (R-JQ1), or DMSO as control. Data, plotted as fold change vs. DMSO, represent the mean ± SEM of 4 independent experiments. * p < 0.05 vs. DMSO. (F) PC-3 cell proliferation was monitored using the IncuCyte live cell analysis system. Cell confluence was calculated from raw data images; the data shown is a representative experiment of 4 biological replicates, and each time point represents mean ± SEM of 4 samples. * p < 0.05 vs. DMSO; # p < 0.05 vs. (R)-JQ1.

Article Snippet: PC-3-luc, 22Rv1-luc, and Du145 cells were treated with the following BET inhibitors and degraders, purchased from MedChemExpress: (S)-(+)-JQ-1 (JQ1, Cat. No.: HY-13030), (R)−(−)−JQ1 (R-JQ1, Cat. No.: HY-13030A), dBET6 (Cat. No.: HY-112588), Bi7273 (Cat. No.: HY-100351), OTX-015 (Cat. No.: HY-15743), and LT052 (Cat. No.: HY-130622).

Techniques: Gene Expression, Control, Cell Analysis

Journal: Frontiers in Pharmacology

Article Title: A Bromodomain-Containing Protein 4 (BRD4) Inhibitor Suppresses Angiogenesis by Regulating AP-1 Expression

doi: 10.3389/fphar.2020.01043

Figure Lengend Snippet: Initial screening of select BET inhibitors to determine their effects on angiogenesis in the chick embryo CAM model. Representative inhibitory results on the growth of blood vessel branches by DMSO (A) or the selected BRD4 inhibitors (B) , which showed strong positive inhibition (+++) of angiogenesis in the chick embryo CAM model. Each BET inhibitors (50 μg/ml) or DMSO was added directly onto the live 9-day-old chick embryo CAM model and incubated for 48 h. Then, the blood vessel network in the chicken embryo CAM was photographed by an OPTPRO 2007 image system. (C) The statistical results of microvessel density (MVD) analysis of the chick embryo CAM model treated with the selected BET inhibitors are shown in Table 1 . (D) Structures of (+)-JQ1 (1) (positive control), ZL0454 (2), MS436 (3), and ZL0513 (7). * P < 0.05 compared with the DMSO group, # P < 0.05 compared with the (+)-JQ1 (1) positive control group.

Article Snippet: The stereoisomer of active (+)-JQ1, (−)-JQ1, which fails to significantly interact with any bromodomain of BET family members and was purchased from MedChemExpress (MCE, Monmouth Junction, NJ, USA) as a negative control.

Techniques: Inhibition, Incubation, Positive Control