JQ1 (+) | BET Bromodomain inhibitor

JQ1 (+) (1268524-70-4) is a potent BET bromodomain inhibitor and is the active isomer.   IC50 = 17.7, 32.6, 76.9 and 12942 nM respectively for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively (data for + isomer).1 Competitive binding by JQ1 displaces the BRD4 fusion oncoprotein from chromatin, prompting squamous differentiation and specific antiproliferative effects in BRD4-dependent cell lines and patient-derived xenograft models.1 Induces squamous differentiation in NMC cell lines and inhibits tumor growth in NMC xenografts.2 Displays reversible contraceptive effects in male mice.3 Blocks inflammation and bone loss in periodontitis.4 Reverses CAR T cell extinction.5

References/Citations

  1. Filippakopoulos et al. (2010), Selective inhibition of BET bromodomains; Nature, 468 1067
  2. Herrmann et al. (2012), Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML; Oncotarget, 3 1588
  3. Matzuk et al. (2012), Small-molecule inhibition of BRDT for male contraception; , 150 673
  4. Meng et al. (2014), BET Inhibitor JQ1 Blocks Inflammation and Bone Destruction;, J. Dent. Res. 93 657
  5. Kong et al. (2021), BET bromodomain protein inhibition reverses chimeric antigen receptor extinction and reinvigorates exhausted T cells in chronic lymphocytic leukemia; Clin. Invest., 131 e145459
Weight 0.01 mg
Dimensions 0.01 × 0.01 × 0.01 cm
size :

5 mg, 25 mg

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CAS:
1268524-70-4
Catalog Number:
10-1584
Activity:
BET Bromodomain inhibitor
Chemical Name:
(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester
Molecular Weight:
456.99
Molecular Formula:
C23H25ClN4O2S
Solubility:
Soluble in DMSO (up to 60 mg/ml) or in Ethanol (up to 46 mg/ml).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT

JQ1 (+) | BET Bromodomain inhibitor

$100.00$400.00

CAS:
1268524-70-4
Catalog Number:
10-1584
Activity:
BET Bromodomain inhibitor
Chemical Name:
(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester
Molecular Weight:
456.99
Molecular Formula:
C23H25ClN4O2S
Solubility:
Soluble in DMSO (up to 60 mg/ml) or in Ethanol (up to 46 mg/ml).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT
  • 5 mg
  • 25 mg
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