2. Epigenetics NF-κB
  3. Histone Acetyltransferase Epigenetic Reader Domain NF-κB
  4. CBP/p300-IN-22

CBP/p300-IN-22 是一种选择性 CBP/EP300 溴结构域抑制剂，IC50 为 4 nM。CBP/p300-IN-22 对BRD4(1) 具有高度选择性。CBP/p300-IN-22 通过抑制 NF-κB 信号传导减少 TNF-α 诱导的细胞因子表达和随后免疫细胞的募集且具有抗癌活性。CBP/p300-IN-22 可用于类风湿性关节炎 (RA) 和其他 TNF-α 介导的炎症疾病的研究[1]。

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CBP/p300-IN-22 Chemical Structure

CBP/p300-IN-22 Chemical Structure

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CBP/p300-IN-22 相关抗体

Top Publications Citing Use of Products

查看 Histone Acetyltransferase 亚型特异性产品:

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CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

CBP/p300-IN-22 (Compound 2) (1 μM，1 小时) 可降低 TNF-α 诱导的 THP-1 细胞中细胞因子 IL-1β、IL-8、MCP-1 和 TNF-α 的表达[1]。

CBP/p300-IN-22 (0-8 小时)能够在 NCI-60 抗增殖筛选中强烈抑制白血病、黑色素瘤和乳腺癌症细胞系的生长[1]。

CBP/p300-IN-22 (0.1-10 μM，3 天) 可能通过降低 MYC 的表达来减少 THP-1 细胞的增殖，且不影响正常细胞[1]。

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

CBP/p300-IN-22 相关抗体:

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
体内研究
(In Vivo)

CBP/p300-IN-22 (160 μM；皮下注射和腹腔注射；注射 rmTNF-α 后 90 分钟) 在 TNF-α 诱导的新型小鼠炎症模型中减少了炎症[1]。

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.
分子量

452.46

Formula

C25H20N6O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CBP/p300-IN-22 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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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产品名称：
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目录号：
HY-176251
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