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Data

Product overview

  • Name
    (+)-JQ1
  • Short description
    Potent, selective BET bromodomain inhibitor. Cell permeable.
  • Biological description

    (+)-JQ1 (JQ1) is a potent, selective and cell permeable inhibitor of the BET (Bromodomain and Extra-Terminal domain) protein family.

    JQ1 selectively binds the BRD2, BRD3, BRD4 and BRDT bromodomain proteins (IC50 values are 17.7, 76.9 and 32.6 nM at BRD2, BRD4(N) and BRD4(C) respectively).


    JQ1 shows highest affinity for BRD4. JQ1 displaces BRD4 from chromatin by competitively binding to the acetyl-lysine recognition pocket to inhibit transcription.


    JQ1 shows effects on tumour growth and survival, cell cycle arrest and differentiation. It has antitumor and anti-angiogenic properties.


    JQ1 shows a short half-life of one hour.

  • Alternative names
    (+)-SGCBD01 | JQ1
  • Biological action
    Inhibitor
  • Purity
    >98%
  • Citations

Properties

  • Chemical name
    (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]di azepine-6-acetic acid 1,1-dimethylethyl ester
  • Molecular Weight
    456.99
  • Chemical structure
    (+)-JQ1  [1268524-70-4]
  • Molecular Formula
    C23H25ClN4O2S
  • CAS Number
    1268524-70-4
  • PubChem identifier
    46907787
  • SMILES
    CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)OC(C)(C)C)C4=CC=C(C=C4)Cl)C
  • Source
    Synthetic
  • InChi
    InChI=1S/C23H25ClN4O2S/c1-12-13(2)31-22-19(12)20(15-7-9-16(24)10-8-15)25-17(11-18(29)30-23(4,5)6)21-27-26-14(3)28(21)22/h7-10,17H,11H2,1-6H3/t17-/m0/s1
  • InChiKey
    DNVXATUJJDPFDM-KRWDZBQOSA-N
  • MDL number
    MFCD22683748
  • Appearance
    Off-white solid

Storing and Using Your Product

  • Storage instructions
    -20°C
  • Solubility overview
    Soluble in DMSO (100mM) and in ethanol (100mM)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for (+)-JQ1

  • Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer.

    Asangani IA et al (2014) Nature 510(7504) : 278-82.
    PubMedID: 24759320
  • Selective inhibition of BET bromodomains.

    Filippakopoulos P et al (2010) Nature 468(7327) : 1067-73.
    PubMedID: 20871596
  • Inhibition of Bromodomain Proteins for the Treatment of Human Diffuse Large B-cell Lymphoma.

    Trabucco SE et al (2015) Clin Cancer Res 21(1) : 113-22.
    PubMedID: 25009295
  • Inhibition of bromodomain proteins for the treatment of human diffuse large B-cell lymphoma.

    Trabucco et al (2015) Clin Cancer res 21(1) : 113-22
    PubMedID: 25009295
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