(-)-JQ1 |
| Katalog-Nr.GC13822 |
A selective inhibitor of BET bromodomains
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1268524-71-5
Sample solution is provided at 25 µL, 10mM.
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(-)-JQ1 is the stereoisomer of JQ1, a cell-permeable small-molecule inhibitor of BET bromodomain that competitively binds to acetyl-lysine recognition motifs. JQ1 is a novel thieno-triazolo-1,4-diazepine with an appended and bulky t-butyl ester functional group at C6 position in its chemical structure, which allows for additional pendant group diversity and mitigates binding to the central benzodiazepine receptor. JQ1 competitively binds to the bromodomain displacing the BRD4 fusion oncoprotein from chromatin, which induces squamous differentiation and specific anti-proliferative effect in BRD4-dependent cell lines and patient-derived xenograft models. However, study results have shown that (-)-JQ1 fails to significantly interact with any bromodomain tested and exhibits inhibition against BRD4(1) with 50% inhibition concentration IC50 value of 10,000 nM.
Reference
[1].Filippakopoulos P, Qi J, Picaud S, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I, Philpott M, Munro S, McKeown MR, Wang Y, Christie AL, West N, Cameron MJ, Schwartz B, Heightman TD, La Thangue N, French CA, Wiest O, Kung AL, Knapp S, Bradner JE. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. doi: 10.1038/nature09504. Epub 2010 Sep 24.
| Cell experiment: [1] | |
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Cell lines |
BRD4-dependent NMC cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
250 nM, 72 hours for proliferation inhibition 250 nM, 48 hours for cell-cycle arrest induction |
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Applications |
In BRD4-dependent NMC cells, differentiation is expectedly accompanied by growth arrest, as demonstrated by reduced Ki67 staining, sustained inhibition of proliferation and G1 cell-cycle arrest. The quantitative RT–PCR for RAD21 and RAN was performed. (-)-JQ1 enantiomer was an inactive control of (+)-JQ1. (+)-JQ1 potently decreased expression of both BRD4 target genes, whereas (-)-JQ1 had no effect. |
| Animal experiment: [1] | |
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Animal models |
Female NCr nude mice bearing NMC 797 xenografts |
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Dosage form |
Intraperitoneal injection, 50 mg/kg, daily |
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Applications |
After 4 days of therapy, mice were evaluated by FDG-PET imaging. A marked reduction in FDG uptake was observed with JQ1 ((+)/-) treatment, whereas vehicle-treated mice demonstrated progressive disease. Tumour-volume measurements confirmed a reduction in tumour growth with JQ1 treatment. JQ1 was well tolerated at this dose and schedule without overt signs oftoxicity or weight loss. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Filippakopoulos P, Qi J, Picaud S, et al. Selective inhibition of BET bromodomains. Nature, 2010, 468(7327): 1067-1073. |
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| Cas No. | 1268524-71-5 | SDF | |
| Chemical Name | (R)-tert-butyl 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 | ||
| Canonical SMILES | CC1=C(C)SC2=C1C(C3=CC=C(Cl)C=C3)=N[C@H](CC(OC(C)(C)C)=O)C4=NN=C(C)N24 | ||
| Formula | C23H25ClN4O2S | M.Wt | 456.99 |
| Löslichkeit | ≥ 22.8mg/mL in DMSO, ≥ 46.9 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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