TPOP146 |
| Katalog-Nr.GC32880 |
TPOP146 ist ein selektiver CBP/P300-Benzoxazepin-BromodomÄnen-Inhibitor mit Kd-Werten von 134 nM und 5,02 μM fÜr CBP und BRD4.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2018300-62-2
Sample solution is provided at 25 µL, 10mM.
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TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
Exposure to 1 μM TPOP146 results in a significant decrease of recovery half-life that is comparable to the construct that contained the bromodomain inactivating mutation N1168F, demonstrating that TPOP146 targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments[1].
[1]. Popp TA, et al. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912.
Kinase experiment: | Proteins are buffered in 10 mM HEPES, pH 7.5, 500 mM NaCl and assayed in a 96-well plate at a final concentration of 2 μM in 20 μL volume. Compounds (TPOP146) are added at a final concentration of 10 μM. SYPRO Orange (Molecular Probes) is added as a fluorescence probe at a dilution of 1:1000. Excitation and emission filters for the SYPRO Orange dye are set to 465 and 590 nm, respectively. The temperature is raised with a step of 3°C per minute from 25 to 96°C, and fluorescence readings are taken at each interval[1]. |
References: [1]. Popp TA, et al. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912. | |
| Cas No. | 2018300-62-2 | SDF | |
| Canonical SMILES | COC1=CC(OC)=CC(C2=CC(C(N[C@H]3CCCN(C)C3)=O)=C(OCCN(C(CC)=O)C4)C4=C2)=C1 | ||
| Formula | C27H35N3O5 | M.Wt | 481.58 |
| Löslichkeit | DMSO : ≥ 100 mg/mL (207.65 mM) | 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 | 2.0765 mL | 10.3825 mL | 20.765 mL |
| 5 mM | 0.4153 mL | 2.0765 mL | 4.153 mL |
| 10 mM | 0.2076 mL | 1.0382 mL | 2.0765 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 9 reference(s) in Google Scholar.)
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