2. Epigenetics NF-κB
  3. Histone Acetyltransferase Epigenetic Reader Domain NF-κB
  4. 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[1].

For research use only. We do not sell to patients.

CBP/p300-IN-22 Chemical Structure

CBP/p300-IN-22 Chemical Structure

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CBP/p300-IN-22 Related Antibodies

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Description

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[1].

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.

CBP/p300-IN-22 Related Antibodies

Cell Viability Assay[1]

Cell Line: THP-1 cells
Concentration: 1 μM, GNE-272 (HY-100726) (1 μM) or A485 (HY-107455) (1 μM) as a control group
Incubation Time: 1 h
Result: Significantly reduced the expression of cytokines IL-1β, IL-8, MCP-1, and TNF-α

Cell Viability Assay[1]

Cell Line: THP-1 and MRC5 cells
Concentration: 0.1-10 μΜ, GNE-272 (HY-100726) (1 μM) or A485 (HY-107455) (1 μM) as a control group
Incubation Time: 3 d
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

CBP/p300-IN-22 (160 μM; s.c. and i.p.; 90 min after injection of rmTNF-α) reduces inflammation in a novel murine model of TNF-α-induced inflammation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Dosage: 160 μM CAPTISOL solutions
Administration: Subcutaneous injection (s.c.) in footpad 10 μL and Intraperitoneal injection (i.p.) 100 μL
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.
Molecular Weight

452.46

Formula

C25H20N6O3
SMILES

CC1=CC2=C(NC(C3=CC(C4=NN(C)C=C4)=CC(NC(C5=CC=CO5)=O)=C3)=O)C=CC=C2N=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CBP/p300-IN-22 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CBP/p300-IN-22Histone AcetyltransferaseEpigenetic Reader DomainNF-κBHATsHATNuclear factor-κBNuclear factor-kappaBCBP/EP300bromodomainNFκBBRD4TNF-αepigeneticsinflammationInhibitorinhibitorinhibit

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