1. Epigenetics Metabolic Enzyme/Protease Immunology/Inflammation
  2. Histone Acetyltransferase Arginase
  3. Conophyllidine

Conophyllidine 是一种双吲哚生物碱,一种选择性的 M2 极化 抑制剂。Conophyllidine 通过作用于 P300/CBP 蛋白的组蛋白乙酰转移酶结构域来抑制组蛋白乙酰化。Conophyllidine 抑制 IL-4 诱导的精氨酸酶 (arginase) 的 IC50 为0.31 μM。Conophyllidine 能够有效地促使肿瘤相关巨噬细胞 (TAMs) 从抗炎型转变为炎症型,从而增强肿瘤微环境中细胞毒性 CD8+T 细胞的募集和功能。Conophyllidine 可用于研究肿瘤相关巨噬细胞。

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Conophyllidine

Conophyllidine Chemical Structure

CAS No. : 152406-44-5

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查看 Histone Acetyltransferase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Conophyllidine, a bisindole alkaloid, is a selective M2 polarization inhibitor. Conophyllidine inhibits histone acetylation by targeting the histone acetyltransferase domain of the P300/CBP proteins. Conophyllidine inhibits IL-4-induced arginase with an IC50 of 0.31 μM. Conophyllidine effectively induces a phenotypic switch in tumor-associated macrophages (TAMs) from an anti-inflammatory to an inflammatory type, thereby enhancing cytotoxic CD8+ T cell recruitment and functionality within the tumor microenvironment. Conophyllidine can be used for the study of TAMs[1].

IC50 & Target[1]

CBP/p300

 

体外研究
(In Vitro)

Conophyllidine (Compound CX-1) (0-1 μM, 12 h) 能够特异性地抑制巨噬细胞 M2 极化,而不会影响 M1 激活[1]
Conophyllidine (Compound CX-1) (0-1 μM, 12 h) 作用于巨噬细胞 P300/CBP 并抑制组蛋白 H3K27 乙酰化[1]

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

Immunofluorescence[1]

Cell Line: Macrophages
Concentration: 0.25, 0.5 and 1 μM
Incubation Time: 12 h
Result: Suppressed IL-4 and induced CD206 expression.
Inhibited IL-4-induced expressions of Arg1, Chil3, Retnla, and Mgl2, as well as LPS-induced expressions of Arg1 and IL10.

Western Blot Analysis[1]

Cell Line: Macrophages
Concentration: 50 μM
Incubation Time: 12 h
Result: Did not affect the expression of P300/CBP.
Interacted with the full-length P300, the BD and HAT domains, and the HAT domain with PEG-biotin.
体内研究
(In Vivo)

Conophyllidine (Compound CX-1) (2 mg/kg, i.p., 一天一次共三天) 通过重新编程 B16F10 黑色素瘤和 4T1 乳腺癌模型中的肿瘤相关巨噬细胞,抑制肿瘤进展并激发小鼠的免疫反应[1]

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

Animal Model: B16F10 melanoma model established in C57BL/6J mice[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 3 days
Result: Significantly delayed tumor growth, prolonged the survival of mice without body weight loss.
Induced upregulation of the macrophage population.
Inhibited the CD206 expression and elevated the MHCII expression.
Upregulated the population of tumor-infiltrating CD8+ T cells and did not affect the population of CD4+ T cells Elevated the expressions of IFNγ, GzmB, and TNFα.
Animal Model: 4T1 breast cancer model established in BALB/c or BALB/c nu/nu mice[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 3 days
Result: Inhibited lung metastasis of breast cancer.
分子量

778.89

Formula

C44H50N4O9

CAS 号
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
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  • 稀释计算器

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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.

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产品名称:
Conophyllidine
目录号:
HY-175180
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