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CBP/p300-IN-22 is a selective inhibitor of the CBP/EP300 bromodomain, with an IC50 of 4 nM. It exhibits high selectivity for BRD4(1) and reduces cytokine expression induced by TNF-α as well as subsequent immune cell recruitment by inhibiting NF-κB signaling, demonstrating anticancer properties. This compound is applicable for research into rheumatoid arthritis (RA) and other TNF-α-mediated inflammatory diseases.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | CBP/p300-IN-22 is a selective inhibitor of the CBP/EP300 bromodomain, with an IC50 of 4 nM. It exhibits high selectivity for BRD4(1) and reduces cytokine expression induced by TNF-α as well as subsequent immune cell recruitment by inhibiting NF-κB signaling, demonstrating anticancer properties. This compound is applicable for research into rheumatoid arthritis (RA) and other TNF-α-mediated inflammatory diseases. |
| Targets&IC50 | p300/CBP:4 nM |
| In vitro | CBP/p300-IN-22 (Compound 2) at a concentration of 1 μM for 1 hour reduces the expression of cytokines IL-1β, IL-8, MCP-1, and TNF-α in TNF-α-induced THP-1 cells. Additionally, CBP/p300-IN-22 strongly inhibits the growth of leukemia, melanoma, and breast cancer cell lines in an NCI-60 antiproliferative screening over a 0-8 hour period. When used at concentrations of 0.1-10 μM for 3 days, it may reduce the proliferation of THP-1 cells by decreasing MYC expression without affecting normal cells. |
| In vivo | CBP/p300-IN-22 (160 μM; subcutaneous and intraperitoneal injections; 90 minutes post rmTNF-α administration) reduced inflammation in a novel mouse model induced by TNF-α. |
| 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.
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