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(+)-JQ1 is a BET bromodomain inhibitor that acts on BRD4(2) with an IC50 of 33 nM and binds to all bromodomain domains in the BET family, but not to bromodomain domains outside the BET family. JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway, and JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway.way.
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Application | growth inhibition assays |
| Results | A subset of lung adenocarcinoma cell lines was also sensitive to bromodomain inhibition with both iBET (Figure S2B) and JQ1 (Figure 2D). |
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Application | growth inhibition assays |
| Results | Debio 1143 was also more effective in combination with the bromodomain inhibitor JQ1. Over a period of 24 hours, Debio 1143 alone induced moderate polyADP ribose polymerase (PARP) cleavage in H1975 and H2030 cells; cleaved PARP levels were greatly enhanced in the presence of JQ1 in H1975 and H2030 cells (Figure 3G). |
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Application | western blot |
| Results | The combination, but neither single agent, elevated IκBα, an NF-κB inhibitor (Figure 4A). Debio 1143, but not JQ1, induced nuclear localization of p52 in each cell line tested - H1975, A549, and H2030, with no augmentation by the combination (Figure 4B, 4C, and 4D). |
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Application | western blot |
| Results | In H1975, H2030, and A549 cells, JQ1 also moderately reduces cIAP1 levels in H1975, A549, and H2030 cells. Protein levels of cIAP1 are undetectable in the Debio 1143/JQ1 combinations (Figure 5A). cIAP2 and XIAP levels were most completely suppressed following combination treatment with Debio 1143 and JQ1 in H1975 cells. Debio 1143 enhanced TNFα mRNA expression in H2030 cells, but not H1975 or A549 (Figure 5B), and JQ1 did not affect TNFα mRNA expression. these results indicate a functioning ripoptosome is formed in the two cell lines most sensitive to the combination of Debio 1143 and JQ1. |
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Application | in vivo |
| Results | Limited effects of the combination of Debio 1143 and JQ1 treatment on tumor volume were observed in H1975 xenografts treated with 30mg/kg Debio 1143; 25mg/kg JQ1 (maximum %treated/control [%T/C] = 52.7%) (Figure 6A). At these drug concentrations, body weights were reduced early in treatment, indicative of toxicity, but body weights stabilized over time (Figure 6B). |
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Application | Treatment started in 4-week-old mice that were euthanized and analyzed at 8 weeks of age. |
| Results | Inhibition of BET bromodomain by JQ1, known to downregulate c-MYC levels in vivo (Delmore et al., 2011), significantly reduced dysplatic lesions in 8-week-old URI(WT)(+/KI)hep livers (Figures 8O–8Q), consistent with the role of c-MYC in liver tumor progression (Qu et al., 2014). |
| Cell Experiment | |
|---|---|
| Cell lines | MM.1S, RPMI-8226, KMS-20, L-363 Dox40 and AMO-1 cell lines |
| Preparation method | Cell Viability Assays MM cell lines were seeded onto 384-well tissue culture treated plates at a density of 1,000 cells/well in a volume of 50 µL of media. After seeding cells were incubated for 1 hour and during the interim a stock plate of JQ1 was thawed at room temperature in a desiccated box. The addition of JQ1 to the assay plate was done with disposable 384-well pins (V&P Scientific, San Diego, CA) that delivered 100 nL of the drug diluted in DMSO to each well of the plate. After 72 hours of incubation cells were analyzed for cell viability by the addition of CellTiter Glo (Promega, Madison, WI) to the assay plates. After 30 min incubation at 37 oC the signal from the viable cells was analyzed on a Luminoskan luminometer (Labsystems Franklin, MA). |
| Concentrations | 0~1µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | SCID-beige mice orthotopically xenografted after intravenous injection with MM.1S-luc+ cells |
| Formulation | JQ1 in 10% cyclodextrine |
| Dosages | 50 mg/kg daily |
| Administration | intra-peritoneally for 5 days/week, 2 weeks |
| Molecular Weight | 456.99 |
| Formula | C23H25ClN4O2S |
| CAS Number | 1268524-70-4 |
| Solubility (25°C) | DMSO 45 mg/mL Ethanol 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Filippakopoulos P, et al. Nature. Selective inhibition of BET bromodomains.
[2] Delmore JE, et al. Cell. BET bromodomain inhibition as a therapeutic strategy to target c-Myc.
[3] Matzuk MM, et al. Cell. Small-molecule inhibition of BRDT for male contraception.
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