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PBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, with dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5 respectively, and an inhibitory concentration 50 (IC50) value of 0.26 μM for PBRM1-BD2. This compound effectively diminishes the interaction between full-length PBRM1 and acetylated histone peptide within the PBAF complex in cell lysates, making it a promising candidate for anticancer research.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $81 | In Stock | |
| 5 mg | $197 | In Stock | |
| 10 mg | $289 | In Stock | |
| 25 mg | $477 | In Stock | |
| 50 mg | $636 | In Stock | |
| 100 mg | $882 | In Stock | |
| 200 mg | $1,180 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $189 | In Stock |
| Description | PBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, with dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5 respectively, and an inhibitory concentration 50 (IC50) value of 0.26 μM for PBRM1-BD2. This compound effectively diminishes the interaction between full-length PBRM1 and acetylated histone peptide within the PBAF complex in cell lysates, making it a promising candidate for anticancer research. |
| 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]. |
| Molecular Weight | 272.73 |
| Formula | C15H13ClN2O |
| Cas No. | 2819989-61-0 |
| Smiles | O=C1C=2C(NC(N1)C3=CC(C)=CC=C3)=CC=CC2Cl |
| Relative Density. | no data available |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (183.33 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.33 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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