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GSK2801 is an effective, specific and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd: 136 nM) and BAZ2B(Kd: 257 nM) bromodomains.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $39 | In Stock | In Stock | |
| 5 mg | $60 | In Stock | In Stock | |
| 10 mg | $79 | In Stock | In Stock | |
| 25 mg | $180 | In Stock | In Stock | |
| 50 mg | $323 | In Stock | In Stock | |
| 100 mg | $538 | In Stock | - | |
| 1 mL x 10 mM (in DMSO) | $63 | In Stock | In Stock |
| Description | GSK2801 is an effective, specific and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd: 136 nM) and BAZ2B(Kd: 257 nM) bromodomains. |
| Targets&IC50 | BAZ2A:257 nM(Kd), BAZ2B:136 nM(Kd) |
| In vitro | In U2OS cells transfected with mutant BAZ2A (N1873F), GSK2801 (1 μM) accelerates FRAP half-recovery time by displacing BAZ2A from chromatin. [1] |
| In vivo | In male CD1 mice, GSK2801 (30 mg/kg, p.o. and i.p.) has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability. [1] |
| Molecular Weight | 371.45 |
| Formula | C20H21NO4S |
| Cas No. | 1619994-68-1 |
| Smiles | CCCOc1ccn2c(cc(-c3ccccc3S(C)(=O)=O)c2c1)C(C)=O |
| Relative Density. | 1.23 g/cm3 (Predicted) |
| 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: 18.6 mg/mL (50.07 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.38 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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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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