1. Epigenetics
    Autophagy
  2. Epigenetic Reader Domain
    Autophagy

(+)-JQ-1 (Synonyms: JQ1)

Cat. No.: HY-13030 Purity: 99.90%
Handling Instructions

(+)-JQ-1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for the first and second bromodomain (BRD4(1/2)).

For research use only. We do not sell to patients.

(+)-JQ-1 Chemical Structure

(+)-JQ-1 Chemical Structure

CAS No. : 1268524-70-4

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10 mM * 1 mL in DMSO USD 77 In-stock
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Customer Review

Other Forms of (+)-JQ-1:

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 28;420:195-207.

    Shh-Light 2 cells are transfected with Gli1 or Gli2 plasmids and the expression of proteins are analyzed by Western blot. Positive control JQ1, CBC and CBD inhibit Gli1 and Gli2 overexpression induced Gli luciferase activity, GDC-0499 and GANT61 have no effects.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Mol Cancer Ther. 2016 Jun;15(6):1217-26.

    JQ1-mediated c-MYC repression correlates with growth inhibition. BETi preferentially inhibit c-MYC protein expression in sensitive cell lines. JQ1-sensitive GP5D, HT29 and LIM1215 cells and JQ1-resistant KM12, SW480 and HuTu80 cells where treated with JQ1 (500 nM) for 2-24 hours and c-MYC protein expression determined by western blot.

    (+)-JQ-1 purchased from MCE. Usage Cited in: J Biol Chem. 2016 Nov 4;291(45):23756-23768.

    BET inhibition blocks growth of TNBC cells without consistently downregulating MYC. Western blot analysis of MYC expression levels in TNBC cell lines treated for 24 hours with vehicle or 500 nM JQ1. Values on the western blot are relative to the vehicle-treated 1143 sample following normalization to β-actin.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2016 Dec;1859(12):1527-1537.

    RVX208 increases CTGF and CYR61 expression and TAZ protein level in HCT116 cells.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2016 Dec;1859(12):1527-1537.

    JQ1 treatment decreases β-catenin levels in HCT116 cells, but increases TAZ protein. When cells reach confluence, they are serum-starved overnight and pretreated with DMSO or JQ1 (500 nM) for 1 hour, followed by growth medium (containing 10% serum) stimulation for 24 hours.

    (+)-JQ-1 purchased from MCE. Usage Cited in: PLoS Pathog. 2016 Oct 20;12(10):e1005950.

    Dose effect of JQ1 on HSV infection. Vero cells are treated with JQ1 at concentrations as indicated. HSV-1 or HSV-2 at 1 MOI are used. The samples are used for protein expression analysis by western blot.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Metabolism. 2016 Oct;65(10):1478-88.

    The BRD4 protein level in the liver is significantly suppressed by force-feeding fructose or glucose with (+)-JQ1. Protein levels of Brd4 in the liver of mice force-fed with glucose or fructose, with or without (+)-JQ1. Quantification of protein levels is performed by normalization against the level of β-actin (n = 6).

    (+)-JQ-1 purchased from MCE. Usage Cited in: J Cell Biochem. 2017 Jan 6.

    JQ1 induces G0/G1 cell cycle arrest and apoptosis of chondrosarcoma cells via regulating p21, p27, Cyclin E2, and Cyclin D1 expression. (A and B) JQ1 regulates the expression of cell cycle regulators such as p21, p27, Cyclin E2, and Cyclin D1. SW 1353 and Hs 819.T cells are seeded into a 6-well plate for 72 h, then the cells are treated with different concentrations of JQ1 (JQ1#1: 200 nM; JQ1#2: 2 μM; JQ1#3: 20 μM) for another 24 h. Total cell lysate is used for the analysis of protein expressio

    (+)-JQ-1 purchased from MCE. Usage Cited in: J Agric Food Chem. 2017 Jun 7;65(22):4384-4394.

    Resveratrol activates the HSF1 signaling pathway. J-Lat A2 cells are treated with various concentrations of Resveratrol or Carfilzomib (50 nM) for 48 h. Then the cells are lysed and Ser320 phosphorylated HSF1 and total HSF1 are detected by Western blot with corresponding antibodies.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Leukemia. 2017 Oct;31(10):2037-2047.

    Immunoprecipitation with anti-BIM antibody illustrates the increased binding of BIM to BCL-2 after JQ1 treatment.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2017 May 31;402:100-109.

    Expression and activation statuses of signal proteins in three BRAFV600E-mutant colon cancer cell lines treated with either Vemurafenib, JQ1, or their combination. Phosphorylation of CRAF and AKT is suppressed by JQ1 in RKO cells and possibly in Colo205 cells (green arrow heads).

    (+)-JQ-1 purchased from MCE. Usage Cited in: J Med Chem. 2017 Jun 22.

    Protein degradation profile of VHL-based BET degraders. Sub-confluent HeLa cells are treated for 24 h with varying concentration of test compounds JQ1(Compound 3), I-BET726 (Compound 4). Protein extracts are separated by SDS-PAGE and then analyzed by Western blot. Proteins Brd4, Brd3, Brd2 and β-actin are probed for JQ1and I-BET726 with specific antibodies.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Genome Res. 2017 Nov;27(11):1830-1842.

    Ki67 immunohistochemistry and H&E stained sections from representative xenograft per treatment arm. A marked decrease in the proliferation marker Ki67 is observed in xenografts treated with JQ1.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.

    The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.

    H3K9Me2, PTEN, p-AKT, and AKT expression levels are measured in PC9/ER xenograft tumor tissues. β-actin is used as a loading control.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Biol Ther. 2018 May 4;19(5):407-415.

    NSCLC cells are treated with 0-8 μM JQ1 for 24h, then the whole-cell lysates are prepared and subjected to western blot assay.

    (+)-JQ-1 purchased from MCE. Usage Cited in: EMBO Mol Med. 2018 Apr;10(4). pii: e8163.

    Western blot analysis of MYC and FGFR3 expression in lysates from MGH-U3 and RT112 cells treated with (+)-JQ1 (1 or 4 μM) for 48 h. Anti-actin antibody is used as a loading control. Pan-FGFR inhibitor, PD173074 (50 nM and 1 μM), and inactive enantiomer (-)-JQ1 (4 μM) are used as controls.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 10;419:64-74.

    ESCC cell lines are treated with 500 nM JQ1 for 48 h, whole cell lysates are analyzed by western blotting. The expressions of p21 and p27 are further upregulated by JQ1 concomitant with cell cycle arrest at G1 phase.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Oncogene. 2018 May 15.

    ARID1A Western blot analysis of ARID1A protein levels in the ES2 polyclonal ARID1A knockout clone and ES2/OVCA429 monoclonal ARID1A knockout clones.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Oncotarget. 2018 May 1;9(33):23003-23017.

    The expression of MYC protein is markedly repressed in JQ1-treated ccRCC cells (2.5 and 5 μM) in comparison with that in mock cells. β-Actin is used as a loading control. Densitometry analyses using ImageJ software are performed.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Jul 29;435:44-54.

    H157, H1299, and HCT116 cells are harvested for preparation of whole-cell protein lysates and subsequent Western blotting to detect the indicated proteins.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Sci Rep. 2018 Aug 1;8(1):11554.

    A549 cells are mock-treated (0.1% DMSO in culture medium) or treated with RVX-208 at 500 nM, PFI-1 at 500 nM, JQ1 at 300 nM, or with 300 nM (-)-JQ1, an inactive enantiomer of JQ1. The cells are then infected with Ad2 at 1 PFU/cell for 24 h. Viral hexon and penton base (PB) protein is detected by immunoblotting analysis.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Aug 28. pii: S0006-2952(18)30368-X.

    The accumulated poly-ubiquitinated protein is detected by Western blotting after J-Lat 10.6 cells are treated with DMSO, PR-957 (100 nM), PR-957 (150 nM) or MG132 (500 nM) for 48 h.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Aug 28. pii: S0006-2952(18)30368-X.

    Western blot detection of the p-TEFb component CDK9, Cyclin T1 and CDK9 phosphorylation on Thr186, as well as its downstream RNA poly II CTD and phosphate CTD after J-Lat 10.6 cells are treated with PR-957 in dose-dependent manner.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Aug 28. pii: S0006-2952(18)30368-X.

    J-Lat 10.6 cells are treated with DMSO, PR-957 (150 nM) or Carfilzomib (40 nM) alone with or without the HSF1 inhibitor KRIBB11 (1.25 µM) for 48 h. Then the cells are lysed, and Ser320 phosphorylated HSF1, total HSF1 and p24 are detected by Western blot with the corresponding antibodies.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Oncogene. 2018 May 15.

    The OVCA429 cells are subjected to Western blot analysis for the indicated proteins. ACTIN servea as a loading control.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cell. 2018 Sep 20;175(1):186-199.e19.

    Cells are treated with EPZ-6438 (1 μM) or GSK126 (1 μM) for 6 days. Protein levels are analyzed by immunoblotting. Cells are treated with EPZ-6438 (1 μM), JQ1 (0.25 μM) alone or combination for 6 days. Protein levels are analyzed by immunoblotting.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    (+)-JQ-1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for the first and second bromodomain (BRD4(1/2)).

    IC50 & Target

    IC50: 77/33 nM (BRD4(1/2))[1]

    In Vitro

    (+)-JQ1 represents a potent, highly specific and Kac competitive inhibitor for the BET family of bromodomains. (+)-JQ1 (100 nM, 48 h) prompts squamous differentiation exhibited by cell spindling, flattening and increased expression of keratin. (+)-JQ1 (250 nM) induces rapid expression of keratin in treated NMC 797 cells compared to (-)-JQ1 (250 nM) and vehicle controls, as determined by quantitative immunohistochemistry.(+)-JQ1 (250 nM) elicits a time-dependent induction of strong (3+) keratin staining of treated NMC 797 cells, compared to (-)-JQ1 (250 nM)[1]. (+)-JQ1 is a potent thienodiazepine inhibitor (Kd=90 nM) of the BET family coactivator protein BRD4, which is implicated in the pathogenesis of cancer via transcriptional control of the MYC oncogene. Dose-ranging studies of (+)-JQ1 demonstrates potent inhibition of H4Kac4 binding with a IC50 value of 10 nM for murine BRDT(1) and 11 nM for human BRDT(1)[2].

    In Vivo

    Matched cohorts of mice with established tumors are randomized to treatment with (+)-JQ1 (50 mg/kg) or vehicle, administered by daily intraperitoneal injection. Prior to randomization, and after four days of therapy, mice are evaluated by FDG-PET imaging. A marked reduction in FDG uptake is observed with (+)-JQ1 treatment. Tumor-volume measurements confirm a reduction in tumor growth with JQ1 treatment. Pharmacokinetic studies of (+)-JQ1 are performed in CD1 mice following intravenous and oral administration. Mean plasma concentration-time profiles of (+)-JQ1 after intravenous dosing (5 mg/kg). The pharmacokinetic parameters for intravenous (+)-JQ1 demonstrate excellent drug exposure (AUC=2090 hr*ng/mL) and an approximately one hour half-life (T1/2). Mean plasma concentration-time profiles of (+)-JQ1 after oral dosing (10 mg/kg). The pharmacokinetic parameters for oral (+)-JQ1 demonstrate excellent oral bioavailability (F=49%), peak plasma concentration (Cmax=1180 ng/mL) and drug exposure (AUC=2090 hr*ng/mL)[1].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 45 mg/mL (98.47 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1882 mL 10.9412 mL 21.8823 mL
    5 mM 0.4376 mL 2.1882 mL 4.3765 mL
    10 mM 0.2188 mL 1.0941 mL 2.1882 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      (+)-JQ-1 (JQ1) is formulated in 10% DMSO and 90% of a 10% 2-hydroxypropyl-β-cyclodextrin solution[3].

    • 2.

      (+)-JQ-1 (JQ1) is prepared in vehicle (20% hydroxypropyl-β-cyclodextrin, 5% DMSO, 0.2% Tween-80 in saline)[4].

    • 3.

      (+)-JQ-1 (JQ1) is prepared in vehicle (1:1 propylene glycol:water)[5].

    • 4.

      (+)-JQ-1 (JQ1) is prepared in vehicle (5% DMSO in 10% 2-hydroxypropyl-β-cyclodextrin solution)[6].

    • 5.

      (+)-JQ-1 is prepared in vehicle (10% hydroxypropyl β-cyclodextrin in water)[7].

    • 6.

      (+)-JQ-1 is freshly dissolved in DMSO and diluted with normal saline (final DMSO at approximately 1%)[8].

    References
    Cell Assay
    [1]

    NUT midline carcinoma patient cell lines (797 and 11060) are plated in T-25 flasks and grown in DMEM (797) or RPMI (11060) containing 10 % fetal bovine serum and 1 % Penicillin/Streptomycin. Cells are treated with either 250 nM (+)-JQ1, 250 nM (-)-JQ1 or the equivalent volume of DMSO (0.025%). At the desired time point, 2×106 cells are spun at 500× g for 5 minutes at 4°C and washed with PBS. Pellets are resuspended in 1 mL of cold PBS and added dropwise while gently vortexing to 9 mL 70 % ethanol in a 15 mL polypropylene centrifuge tube. Fixed cells are then frozen at -20°C overnight. The next day, cells are centrifuged at 500× g for 10 minutes at 4°C and washed with 3 mL of cold PBS. Cells are resuspended in 500 μL of propidium iodide staining solution (0.2 mg/mL RNAse A, 0.02 mg/mL propidium iodide, 0.1 % Triton-X in PBS) and incubated for 20 minutes at 37°C. Samples are then transferred to ice and analyzed on a BD FACS Canto II. Histograms are generated and cell cycle analysis is performed using FlowJo flow cytometry analysis software[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1][2]

    Mice[1]
    Matched cohorts of mice with established tumors are randomized to treatment with (+)-JQ1 (50 mg/kg) or vehicle, administered by daily intraperitoneal injection. Male CD1 mice (24-29 g) are treated with a single dose of (+)-JQ1 at 5 mg/kg for intravenous tail vein injection studies and 10 mg/kg for oral gavage studies. Approximately 150 μL of blood are taken from animals by retro-orbital puncture under anesthesia with Isoflurane into EDTA tubes at pre-specified time intervals: 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 5, 8 and 24 hours. Three animals are analyzed per time point. Blood samples are put on ice and centrifuged to obtain plasma samples (2000× g, 5 min under 4°C) within 15 minutes post-sampling. Plasma samples are stored at approximately -70°C until analysis is performed. Mice are provided free access to food and water throughout the study.
    Rats[2]
    Adult male Sprague-Dawley rats are treated with vehicle or (+)-JQ1 (10 mg/kg). Treatment is administered IP at 1/100 body mass. Rats are checked twice-daily for mortality and weighed on days 1, 3, 7, 14, and 21. The treatment regimen utilized 4 days of 50 mg/kg JQ1 administered daily which is decreased to 10 mg/kg twice daily for the remainder of the study due to the appearance of adverse effects in a subset of animals. For all animals completing 3 weeks of treatment, testis mass, sperm motility, and sperm counts are determined as described for mouse studies. In brief, testes are fixed in Bouin’s and prepared for histology. The other half is minced in warm M16 buffer and used for sperm counts and motility studies.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    456.99

    Formula

    C₂₃H₂₅ClN₄O₂S

    CAS No.

    1268524-70-4

    SMILES

    O=C(C[[email protected]]1C2=NN=C(N2C3=C(C(C4=CC=C(C=C4)Cl)=N1)C(C)=C(S3)C)C)OC(C)(C)C

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.90%

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    Product Name:
    (+)-JQ-1
    Cat. No.:
    HY-13030
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    (+)-JQ-1

    Cat. No.: HY-13030