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BRD4/CK2-IN-1 is a small molecule inhibitor targeting BRD4 and CK2, with an IC50 of 180nM for BRD4 and 230nM for CK2. It inhibits the proliferation of MDA-MB-231 and MDA-MB-468 cells, inducing apoptosis and autophagy-related cell death. It can be used in triple-negative breast cancer research.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $84 | - | In Stock | |
| 5 mg | $198 | - | In Stock | |
| 10 mg | $313 | - | In Stock | |
| 25 mg | $619 | - | In Stock | |
| 50 mg | $987 | - | In Stock | |
| 100 mg | $1,490 | - | In Stock | |
| 200 mg | $1,970 | - | In Stock |
| Description | BRD4/CK2-IN-1 is a small molecule inhibitor targeting BRD4 and CK2, with an IC50 of 180nM for BRD4 and 230nM for CK2. It inhibits the proliferation of MDA-MB-231 and MDA-MB-468 cells, inducing apoptosis and autophagy-related cell death. It can be used in triple-negative breast cancer research. |
| Targets&IC50 | CK2:230 nM, BRD4:180 nM |
| In vitro | BRD4/CK2-IN-1 showed significant inhibitory activity against BRD4 (IC50 = 180 nM). BRD4/ CK2-in-1 showed significant inhibitory activity against CK2 (IC50 = 230 nM). BRD4/ CK2-in-1 induces TNBC cell death by targeting BRD4 and CK2. BRD4/ CK2-in-1 can bind to BRD4 and CK2 IN cells and inhibit BRD4 and CK2-regulated proliferation pathways, but has no significant effect on the protein levels of BRD4 and CK2. [1] |
| In vivo | In MDA-MB-468 and MDA-MB-231 xenograft tumor models, BRD4/CK2-IN-1 (25 mg/kg and 50 mg/kg) was administered intravenously and orally to inhibit tumor growth in a dose-dependent manner. [1] |
| Molecular Weight | 564.03 |
| Formula | C29H30ClN5O5 |
| Cas No. | 2756851-99-5 |
| Smiles | O=C1N=C(NC=2C=C(OC)C=C(OC)C12)C=3C=CC(OCC(=O)NC4=CC=C(C(Cl)=C4)N5CCN(C)CC5)=CC3 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 16 mg/mL (28.37 mM), when pH is adjusted to 3 with HCl, sonication is recommended. | |||||||||||||||||||||||||
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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