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
Description
IC50 & Target
[1]|
CBP/p300 4 nM (IC50) |
BRD4(1) 3.7 μM (Kd) |
In Vitro
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
In Vivo
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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