1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. FOXM1-IN-4

FOXM1-IN-4 是一种选择性的 5-HT7 受体抑制剂,其 Ki 值为 92 nM。FOXM1-IN-4 可阻断 5-HT7 受体信号通路,从而降低 FOXM1p-FOXM1cyclin B1cdc25B 的表达水平。FOXM1-IN-4 具有抗增殖、克隆形成抑制及细胞周期抑制活性,可诱导 G2/M 期阻滞,减少 G0/G1 期细胞占比。FOXM1-IN-4 可用于三阴性乳腺癌的相关研究。

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FOXM1-IN-4

FOXM1-IN-4 Chemical Structure

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Other Forms of FOXM1-IN-4:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FOXM1-IN-4 is a selective 5-HT7 receptor inhibitor with a Ki of 92 nM. FOXM1-IN-4 blocks 5-HT7 receptor signaling to reduce FOXM1, p-FOXM1, cyclin B1, and cdc25B levels. FOXM1-IN-4 acts as an antiproliferative, clonogenic inhibitor, and cell cycle inhibitor that induces G2/M arrest, reduces G0/G1 population. FOXM1-IN-4 can be used for the research of triple-negative breast cancer[1].

IC50 & Target[1]

5-HT7 Receptor

92 nM (Ki)

5-HT7 Receptor

11 nM (Kb)

体外研究
(In Vitro)

FOXM1-IN-4 (Compound 36) 可与 HEK293 细胞中表达的 5-HT7 受体紧密结合,其 Ki 为 92 nM,Kb 为 11 nM[1]
FOXM1-IN-4 (0.1-315.5 μM;24 小时) 可强效抑制 MDA-MB-468、MDA-MB-231 和 Hs578T 三阴性乳腺癌 (TNBC) 细胞的增殖,其 IC50 值分别为 7.1 μM、11.3 μM 和 6.7 μM;同时对 NHDF 细胞的细胞毒性有限,IC50 值为 12.2 μM[1]
FOXM1-IN-4 (0.7-6.7 μM;7 天) 以剂量依赖的方式抑制 MDA-MB-231 和 Hs578T 三阴性乳腺癌 (TNBC) 细胞的长期克隆形成能力[1]
FOXM1-IN-4 (16.95 μM;24 小时) 处理 MDA-MB-231 三阴性乳腺癌 (TNBC) 细胞,可诱导细胞周期阻滞于 G2/M 期[1]
FOXM1-IN-4 (16.95 μM;24 小时) 可在以 1.5 × IC50 处理 MDA-MB-231 三阴性乳腺癌 (TNBC) 细胞 24 h 后,抑制 FOXM1 激活及下游 G2/M 期调控因子 (cyclin B1、cdc25B) 的表达[1]
FOXM1-IN-4 (5.63-22.6 μM;24 小时) 在经血清素 (10-20 μM; 48 h) 预处理的 MDA-MB-231 三阴性乳腺癌 (TNBC) 细胞中展现出增强的抗增殖活性,其中经 20 μM 血清素预处理时的效果最强[1]

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

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, Hs578T (TNBC cell lines)
Concentration: 0.7 μM; 1.4 μM; 2.8 μM; 5.7 μM; 0.8 μM; 1.7 μM; 3.4 μM; 6.7 μM
Incubation Time: 7 days
Result: Significantly and dose-dependently reduced colony formation in both cell lines.
In MDA-MB-231 cells, the highest tested concentration (5.7 μM) caused the strongest reduction in colony numbers, with weaker effects at lower doses.
In Hs578T cells, reduced clonogenic growth at higher concentrations, with statistically significant inhibitory effects observed.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231, Hs578T (TNBC cell lines)
Concentration: 16.95 μM
Incubation Time: 24 h
Result: In MDA-MB-231 cells, caused a marked decrease in the proportion of cells in the G0/G1 phase and a modest increase in the G2/M phase population, inducing cell cycle arrest.

Western Blot Analysis[1]

Cell Line: MDA-MB-231, Hs578T (TNBC cell lines)
Concentration: 16.95 μM
Incubation Time: 24 h
Result: In MDA-MB-231 cells, reduced total FOXM1 expression by over 2.6-fold and reduced p-FOXM1 levels by approximately 2.7-fold.
Caused a reduction in cyclin B1 and cdc25B protein levels in MDA-MB-231 cells.
分子量

456.59

Formula

C26H32N8

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
  • 摩尔计算器

  • 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:
FOXM1-IN-4
目录号:
HY-182285
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