CBP/p300-IN-22
CBP/p300-IN-22 is a selective CBP/EP300-BRD inhibitor with an IC50 of 4 nM. CBP/p300-IN-22 is highly selective over BRD4(1). CBP/p300-IN-22 reduces TNF-α-induced cytokine expression and subsequent immune cell recruitment by inhibiting NF-κB signaling, and has anticancer activity. CBP/p300-IN-22 can be used for the research of rheumatoid arthritis (RA) and other TNF-α-mediated inflammatory conditions.
For research use only. We do not sell to patients.
- Formula: C25H20N6O3
- Molecular Weight:452.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CBP/p300 4 nM (IC50) |
BRD4(1) 3.7 μM (Kd) |
CBP/p300-IN-22 (Compound 2) (1 μM, 1 h) reduces the expression of cytokines IL-1β, IL-8, MCP-1, and TNF-α in THP-1 cells induced by TNF–α [1].
CBP/p300-IN-22 (0-8 h) is able to strongly inhibit the growth of leukemia, melanoma and breast cancer cell lines in the NCI-60 antiproliferation screen [1].
CBP/p300-IN-22 (0.1-10 μM, 3 d) reduces the proliferation of THP-1 cells possibly by lowering the expression of MYC, instead of non-cancerous cells [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 cells
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Concentration:1 μM, GNE-272 (HY-100726) (1 μM) or A485 (HY-107455) (1 μM) as a control group
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Incubation Time:1 h
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Result:Significantly reduced the expression of cytokines IL-1β, IL-8, MCP-1, and TNF-α
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Cell Line:THP-1 and MRC5 cells
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Concentration:0.1-10 μΜ, GNE-272 (HY-100726) (1 μM) or A485 (HY-107455) (1 μM) as a control group
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Incubation Time:3 d
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Result:Reduced the proliferation of THP-1 cells, but did not cause a decrease in the proliferation of MRC5 cells. And A485 could cause MRC5 cells death
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The inflammation model was constructed by subcutaneous injection of 300 ng of recombinant murine TNF-α (rmTNF-α) into C57BL/6 mice[1].
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Dosage:160 μM CAPTISOL solutions
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Administration:Subcutaneous injection (s.c.) in footpad 10 μL and Intraperitoneal injection (i.p.) 100 μL
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Result:Reduced the concentration of inflammatory cytokines IL-1β, MCP-1, IL-1α and IL-6.
Significantly inhibited the recruitment of lymphocytes, dendritic cells and neutrophils.
Chemical Information
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Molecular Weight 452.46
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Formula C25H20N6O3
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SMILES
CC1=CC2=C(NC(C3=CC(C4=NN(C)C=C4)=CC(NC(C5=CC=CO5)=O)=C3)=O)C=CC=C2N=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CBP/p300-IN-22 Related Classifications
HY-176251 Related Classifications
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