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Synonyms:
P300-IN-6
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | P300-IN-6 is an orally active inhibitor of the histone acetyltransferase (HAT) p300 domain, with an IC50 value of 7 nM in humans. It suppresses c-Myc expression, reduces H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation. Additionally, P300-IN-6 hinders tumor growth in xenograft mouse models and is suitable for research in multiple myeloma. |
| Targets & IC50 | p300 HAT:7 nM |
| In vitro | P300-IN-6 (Compound B6) is a potent inhibitor of the recombinant human p300 HAT domain, with an IC₅₀ of 7 nM. It effectively suppresses the proliferation of human multiple myeloma OPM-2 cells, showing an IC₅₀ of 8.8 nM. At a concentration of 100 nM over six days, P300-IN-6 achieves 70-80% growth inhibition of human prostate cancer 22RV1 cells. Additionally, in the range of 1-20 nM over 24 hours, it dose-dependently inhibits c-Myc expression and reduces H3K18ac/H3K27ac levels in OPM-2 and 22RV1 cells. |
| In vivo | P300-IN-6 (Compound B6) administered at a dose of 20 mg/kg via gavage once daily for 17 days achieved 60% tumor growth inhibition in the OPM-2 multiple myeloma xenograft model in mice. |
| Molecular Weight | 454.52 |
| Formula | C26H26N6O2 |
| Cas No. | 3034595-62-2 |
| Smiles | CN1C=2C(=CC=C(NC([C@H](NC[C@@H](C)C3=CC=C(C#N)C=C3)C4=CC=CC=C4)=O)N2)N(C)C1=O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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.
| Size | Quantity | Unit Price | Amount | Operation |
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