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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 | $88 | In Stock | |
2 mg | $127 | In Stock | |
5 mg | $198 | In Stock | |
10 mg | $317 | In Stock | |
25 mg | $477 | In Stock | |
50 mg | $636 | In Stock | |
100 mg | $882 | In Stock | |
500 mg | $1,770 | 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 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (183.33 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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