PBRM1-BD2-IN-5
Based on 1 Customer Validation
PBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with Kd values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.26 μM for PBRM1-BD2. PBRM1-BD2-IN-5 reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptide. PBRM1-BD2-IN-5 can be used to research anticancer.
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- Pureté: 99.75%
- CAS No.: 2819989-61-0
- Formule: C15H13ClN2O
- Masse moléculaire:272.73
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
Kd: 1.5 μM (PBRM1-BD2), 3.9 μM (PBRM1-BD5)[1]
IC50: 0.26 μM (PBRM1-BD2)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
8.8 μM
Compound: 16
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Cytotoxicity against human LNCaP cells assessed as inhibition of cell growth measured after 7 days with compound replacement for every 48 hrs by celltiter-glo assay
Cytotoxicity against human LNCaP cells assessed as inhibition of cell growth measured after 7 days with compound replacement for every 48 hrs by celltiter-glo assay
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[PMID: 36227159] |
In Vitro
PBRM1-BD2-IN-5 (compound 16) (0-10 μM; 5 days) inhibits PBRM1-expressed LNCaP cells, and reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP cells expressing lentiviral shPBRM1
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Concentration:0, 0.1, 1 and 10 μM
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Incubation Time:5 days
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Result:Exhibited a more significant effect on LNCaP viability in cells with native PBRM1 levels than in cells with PBRM1 knockdown.
Reduced the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides.
Chemical Information
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CAS No. 2819989-61-0
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Appearance Solid
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Masse moléculaire 272.73
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Formule C15H13ClN2O
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Color White to off-white
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SMILES
O=C1NC(C2=CC=CC(C)=C2)NC3=C1C(Cl)=CC=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (366.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.6666 mL | 18.3331 mL | 36.6663 mL | 91.6657 mL |
| 5 mM | 0.7333 mL | 3.6666 mL | 7.3333 mL | 18.3331 mL | |
| 10 mM | 0.3667 mL | 1.8333 mL | 3.6666 mL | 9.1666 mL | |
| 15 mM | 0.2444 mL | 1.2222 mL | 2.4444 mL | 6.1110 mL | |
| 20 mM | 0.1833 mL | 0.9167 mL | 1.8333 mL | 4.5833 mL | |
| 25 mM | 0.1467 mL | 0.7333 mL | 1.4667 mL | 3.6666 mL | |
| 30 mM | 0.1222 mL | 0.6111 mL | 1.2222 mL | 3.0555 mL | |
| 40 mM | 0.0917 mL | 0.4583 mL | 0.9167 mL | 2.2916 mL | |
| 50 mM | 0.0733 mL | 0.3667 mL | 0.7333 mL | 1.8333 mL | |
| 60 mM | 0.0611 mL | 0.3056 mL | 0.6111 mL | 1.5278 mL | |
| 80 mM | 0.0458 mL | 0.2292 mL | 0.4583 mL | 1.1458 mL | |
| 100 mM | 0.0367 mL | 0.1833 mL | 0.3667 mL | 0.9167 mL |
PBRM1-BD2-IN-5 Related Classifications
HY-151532 Related Classifications
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