Product overview

Name (+)-JQ1
Alternative names (+)-SGCBD01 | JQ1
Purity >98%
Description Potent, selective BET bromodomain inhibitor. Cell permeable.
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Biological Data

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.

Solubility & Handling

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.

Calculators

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Dilution

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Chemical Data

Purity >98%
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] Chemical Structure
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

References for (+)-JQ1

References are publications that support the biological activity of the product
  • 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
  • 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.
  • Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer.

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

    Filippakopoulos P et al (2010) Nature 468(7327) : 1067-73.

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