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(+)-JQ1

Cat. No. M2167
(+)-JQ1 Structure
Size Price Availability Quantity
10mg USD 165 In stock
50mg USD 250 In stock
100mg USD 400 In stock
200mg USD 700 In stock
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Quality Control
Biological Activity

(+)-JQ1 binds to all bromodomains of the BET family with IC50 values of 17.7, 32.6, 76.9 and 12942 nM for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively; Kd values of 49, 59.5, 82, 90.1, 128 and 190 nM for BRD4 (N), BRD3 (N), BRD3 (C), BRD4 (C), BRD2 (N) and BRDT (N) respectively. (+)-JQ1 inhibits tumor growth in NMC xenograft models in vivo. (+)-JQ1 induces squamous differentiation in NUT midline carcinoma (NMC) cell lines. The BET bromodomain inhibitor (+)-JQ1 (5 μM) dissociates Brd4 from the HIV promoter to allow Tat recruitment of SEC to stimulate HIV elongation. (+)-JQ1 has been used as a chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis. (+)-JQ1 (50 mg/kg i.p.) leads to a highly significant increase in survival of mice bearing Raji xenografts. (+)-JQ1 is more effective than (-)-JQ1.

Protocol
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 (Sigma)
Dosages 50 mg/kg daily
Administration intra-peritoneally for 5 days/week, 2 weeks
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 456.99
Formula C23H25ClN4O2S
CAS Number 1268524-70-4
Purity 100.00%
Solubility DMSO
Ethanol
Storage at -20°C
Customer Product Validations & Biological Datas
Source Cancer Cell (2016). Figure 8. (+)-JQ1 (Abmole Bioscience, Shanghai, China)
Method Treatment started in 4-week-old mice that were euthanized and analyzed at 8 weeks of age.
Cell Lines
Concentrations 50 mg/kg
Incubation Time
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).
Rating
Source Oncotarget.(2015) . Figure 6. JQ1 (Abmole Bioscience)
Method in vivo
Cell Lines H1975 and A549 lung adenocarcinoma in xenograft mouse models
Concentrations 25 mg/kg i.p.
Incubation Time 20 days
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).
Rating
Source Oncotarget.(2015) . Figure 5. JQ1 (Abmole Bioscience)
Method western blot
Cell Lines A549, H1975, H2030 cells
Concentrations 1000 nM
Incubation Time 24 h
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.
Rating
Source Oncotarget.(2015) . Figure 4. JQ1 (Abmole Bioscience)
Method western blot
Cell Lines A549, H1975, H2030 cells
Concentrations 1000 nM
Incubation Time 24 h
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).
Rating
Source Oncotarget.(2015) . Figure 3. JQ1 (Abmole Bioscience)
Method growth inhibition assays
Cell Lines A549, H1975, H2030 cells
Concentrations 0~100 µ M
Incubation Time 24 h
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).
Rating
Source Oncotarget.(2015) . Figure 2. JQ1 (Abmole Bioscience)
Method growth inhibition assays
Cell Lines A549, H1650, H1975, H820, H2030 and H2228 cells
Concentrations 0~10 µ M
Incubation Time 24 h
Results A subset of lung adenocarcinoma cell lines was also sensitive to bromodomain inhibition with both iBET (Figure S2B) and JQ1 (Figure 2D).
Rating
Product Citations
References

The BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation.
Li Z, et al. Nucleic Acids Res. 2013 Jan 7;41(1):277-87. PMID: 23087374.

Small-molecule inhibition of BRDT for male contraception.
Matzuk MM, et al. Cell. 2012 Aug 17;150(4):673-84. PMID: 22901802.

BET bromodomain inhibition as a therapeutic strategy to target c-Myc.
Delmore JE, et al. Cell. 2011 Sep 16;146(6):904-17. PMID: 21889194.

Selective inhibition of BET bromodomains.
Filippakopoulos P, et al. Nature. 2010 Dec 23;468(7327):1067-73. PMID: 20871596.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: (+)-JQ1 supplier, Epigenetic Reader Domain, inhibitors

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