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    InvivoChem Cat #: V0411
    CAS #: 1268524-70-4 Purity ≥98%

    Description: (+)-JQ1 is a novel, potent and highly specific BET (Bromodomain and extra terminal domain) bromodomain inhibitor with antineoplastic activity. It inhibits BRD4(1/2) with an IC50 of 77 nM and 33 nM in enzymatic assays. It has high specificity for BET in that it only binds to bromodomains of the BET family, but not to any bromodomains of non-BET family. (+)-JQ1 has potential antineoplastic activity against various cancers such as MM (Multiple myeloma), pancreatic ductal adenocarcinoma and ovarian cancer etc. Its mechanism of action is to inhibit c-MYC and upregulate p21. (+)-JQ1 has been used as a chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis.

    References: Nature. 2010 Dec 23;468(7327):1067-73; Cell. 2011 Sep 16;146(6):904-17; Proc Natl Acad Sci U S A. 2011 Oct 4;108(40):16669-74.

    Related CAS: 1268524-71-5 [(-)-JQ-1]; 202592-23-2 [(+)-JQ1 carboxylic acid]; 2115701-93-2 [(+)-JQ1 PA]; 

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    Molecular Weight (MW)456.99
    CAS No.1268524-70-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 91 mg/mL (199.1 mM)
    Water: <1 mg/mL
    Ethanol:  91 mg/mL (199.1 mM)
    Solubility (In vivo)2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
    SynonymsBromodomain Inhibitor; (+)-JQ 1; (+)-JQ-1; (+)-JQ1; 
    SMILES CodeO=C(OC(C)(C)C)C[[email protected]]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1
    Chemical Nametert-butyl (S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl) acetate

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    In Vitro

    In vitro activity: (+)-JQ1 enantiomer binds directly into the Kac binding site of BET bromodomains. (+)-JQ1 (500 nM) binds BRD4 competitively with chromatin resulting in differentiation and growth arrest of NMC cells. (+)-JQ1 (500 nM) attenuates rapid proliferation of NMC 797 and Per403 cell lines as demonstrated by reduced Ki67 staining. (+)-JQ1 (500 nM) potently decreases expression of both BRD4 target genes in NMC 797 cells. (+)-JQ1 inhibits cellular viability with IC50 of 4 nM in NMC 11060 cells. (+)-JQ1 results in robust inhibition of MYC expression in MM cell lines. (+)-JQ1 inhibits proliferating of KMS-34 and LR5 with IC50 of 68 nM and 98 nM, respectively. (+)-JQ1 (500 nM)-treated MM.1S cells results in a pronounced decrease in the proportion of cells in S-phase, with a concomitant increase in cells arrested in G0/G1. (+)-JQ1 (500 nM) results in pronounced cellular senescence by beta-galactosidase staining. (+)-JQ1 (800 nM) exposure leads to a significant reduction in cell viability among the majority of CD138+ patient-derived MM samples tested. (+)-JQ1 inhibits growth of LP-1 cells with GI50 of 98 nM. (+)-JQ1 (625 nM) results in an increase in the percentage of LP-1 cells in G0/G1. (+)-JQ1 (500 nM) suppresses the expression of MYC, BRD4 and CDK9 in LP-1 cells. (+)-JQ1 (1 μM) activates HIV transcription in latently infected Jurkat T cells. (+)-JQ1 (50 μM) stimulates predominantly Tat-dependent HIV transcription in both Jurkat and HeLa cells. (+)-JQ1 (5 μM) induces Brd4 dissociation enables Tat to recruit SEC to HIV promoter and induce Pol II CTD phosphorylation and viral transcription in J-Lat A2 cells. JQ1 enables Tat to increase CDK9 T-loop phosphorylation and partially dissociates P-TEFb from 7SK snRNP in Jurkat T cells.

    Kinase Assay: (+)-JQ1 is a potent and highly specific BET (Bromodomain and extra terminal domain) bromodomain inhibitor, with IC50 of 77 nM and 33 nM for BRD4(1/2) in enzymatic assays.

    Cell Assay: Cells are seeded into white, 384-well microtiter plates at 500 cells per well in a total volume of 50 μL media. The 797, TT and TE10 cells are grown in DMEM containing 1% penicillin/streptomycin and 10% FBS. The Per403 cells are grown in DMEM containing 1 % penicillin/streptomycin and 20% FBS. Patient-derived NMC 11060 cells are grown in RPMI with 10% FBS and 1% penicillin/streptomycin. (+)-JQ1 is delivered to microtiter assay plates by robotic pin transfer. Following a 48 hours incubation at 37℃, cells are lysed and wells are assessed for total ATP content using a commercial proliferation assay. Replicate measurements are analyzed with respect to dose and estimates of IC50 are calculated by logistic regression (GraphPad Prism).

    In Vivo(+)-JQ1 (50 mg/kg) inhibits tumors growth in mice with NMC 797 xenografts. (+)-JQ1 (50 mg/kg) results in effacement of NUT nuclear speckles in mice with NMC 797 xenografts, consistent with competitive binding to nuclear chromatin. (+)-JQ1 (50 mg/kg) induces strong (grade 31) keratin expression in NMC 797 xenografts. (+)-JQ1 (50 mg/kg) promotes differentiation, tumor regression and prolonged survival in mice models of NMC xenografts. (+)-JQ1 (50 mg/kg) results in a significant prolongation in overall survival of SCID-beige mice orthotopically xenografted after intravenous injection with MM.1S-luc+ cells compared to vehicle-treated animals. (+)-JQ1 (50 mg/kg i.p.) leads to a highly significant increase in survival of mice bearing Raji xenografts.
    Animal modelMice bearing NMC 797 xenografts
    Formulation & Dosage1. Dissolved in 5% dextrose; 50 mg/kg; i.p. injection; Nature. 2010 Dec 23;468(7327):1067-73;
    2. Dissolved in 10% DMSO and 90% of a 10% 2-hydroxypropyl-β-cyclodextrin solution; Leukemia. 2017 Oct;31(10):2037-2047.;
    3. Dissolved in 1% DMSO+5% Glucose+ddH2O; Cell. 2018 Sep 20;175(1):186-199.e19.;
    4. Dissolved in 20% hydroxypropyl-β-cyclodextrin, 5% DMSO, 0.2% Tween-80 in saline; Mol Cancer Ther. 2016 Jun;15(6):1217-26.;
    5. Dissolved in 1:1 propylene glycol:water; J Biol Chem. 2016 Nov 4;291(45):23756-23768.;
    6. Dissolved in 5% DMSO in 10% 2-hydroxypropyl-β-cyclodextrin solution; Cancer Lett. 2017 Aug 28;402:100-109.
    References Nature. 2010 Dec 23;468(7327):1067-73; Cell. 2011 Sep 16;146(6):904-17; Proc Natl Acad Sci U S A. 2011 Oct 4;108(40):16669-74.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


    Leukemia and lymphoma cell lines are broadly sensitive to BET-bromodomain inhibition.  2011 Oct 4;108(40):16669-74.


    Gene expression profiling of LP-1 and Raji cells treated with active or inactive BET inhibitors.  2011 Oct 4;108(40):16669-74.


    Small molecule BET-bromodomain inhibition suppresses MYC transcription.  2011 Oct 4;108(40):16669-74.


    MYC reconstitution significantly protects cells from BET-mediated effects.  2011 Oct 4;108(40):16669-74.


    BET-bromodomain inhibition decreases tumor load in vivo.  2011 Oct 4;108(40):16669-74.


    Integrated genomic rationale for BET bromodomains as therapeutic targets in MM.  2011 Sep 16;146(6):904-17.


    Inhibition of Myc-dependent transcription by the JQ1 BET bromodomain inhibitor.  2011 Sep 16;146(6):904-17.


    BET inhibition suppresses MYC transcription in MM.  2011 Sep 16;146(6):904-17.


    Regulation of MYC transcription by BET bromodomains.  2011 Sep 16;146(6):904-17.


    Anti-myeloma activity of JQ1 in vitro.  2011 Sep 16;146(6):904-17. 


    JQ1 induces cell cycle arrest and cellular senescence in MM cells.  2011 Sep 16;146(6):904-17.


    Translational implications of BET bromodomain inhibition in MM.  2011 Sep 16;146(6):904-17.




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