2. PI3K/Akt/mTOR Cell Cycle/DNA Damage Apoptosis
  3. PI3K CDK Apoptosis
  4. FOXM1-IN-3

FOXM1-IN-3 是一种强效的 FOXM1 抑制剂，同时为弱效的 PI3Kγ 抑制剂 (IC50 为 3.5 μM)。FOXM1-IN-3 在蛋白和 mRNA 水平下调 FOXM1 表达，抑制下游效应因子 CCNB1 和 CDC25。FOXM1-IN-3 可诱导结直肠癌细胞发生 G2/M 期细胞周期阻滞和凋亡 (apoptosis)。FOXM1-IN-3 抑制结直肠癌细胞的集落形成能力和细胞迁移能力。FOXM1-IN-3 靶向结直肠癌细胞的癌症干细胞表型，降低癌症干细胞标志物的表达。FOXM1-IN-3 在斑马鱼异种移植模型中抑制肿瘤生长。FOXM1-IN-3 可用于结直肠癌研究。

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FOXM1-IN-3

FOXM1-IN-3 Chemical Structure

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FOXM1-IN-3 相关抗体

Top Publications Citing Use of Products

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FOXM1-IN-3 is a potent FOXM1 inhibitor and a weak PI3Kγ inhibitor (IC50 of 3.5 μM). FOXM1-IN-3 downregulates FOXM1 expression at protein and mRNA levels, suppressing downstream effectors CCNB1 and CDC25. FOXM1-IN-3 induces G2/M cell cycle arrest and apoptosis in colorectal cancer cells. FOXM1-IN-3 inhibits colony formation and cell migration in colorectal cancer cells. FOXM1-IN-3 targets the cancer stem cell phenotype in colorectal cancer cells, reducing cancer stem cell marker expression. FOXM1-IN-3 reduces tumor growth in a zebrafish xenograft model. FOXM1-IN-3 can be used for the research of colorectal cancer[1].

IC50 & Target

FOXM1

 

PI3Kγ

3.5 μM (IC50)

体外研究
(In Vitro)

FOXM1-IN-3 (compound 14) (6.25-100 μM；作用 24 h) 可强效抑制 SW620 和 SW480 结直肠癌细胞的增殖，其 IC50 值分别为 14.9 μM 和 17.5 μM，且相对于正常 CCD841 细胞 (IC50 为 36.65 μM) 表现出良好的选择性[1]。
FOXM1-IN-3 (0.75-3 μM；作用 7 天) 在 3 μM 浓度下几乎完全抑制 SW480 和 SW620 细胞的集落形成，体现出长期抗增殖效应[1]。
FOXM1-IN-3 (6.25-25 μM；作用 48 h) 可在 48 h 内以 6.25 μM 的浓度抑制 SW480 细胞的迁移，以 12.5 μM 的浓度抑制 SW620 细胞的迁移[1]。
FOXM1-IN-3 对 PI3Kβ、γ 和 δ 均表现出可测量的抑制作用，其中对 PI3Kδ 的抑制作用最为显著 (IC50 为 3.5 μM)[1]。
FOXM1-IN-3 (6.25-25 μM；作用 24 小时) 在低至 6.25 μM 的浓度下，可下调 SW480 和 SW620 细胞中的 FOXM1 及其下游效应因子 CCNB1 与 CDC25[1]。
FOXM1-IN-3 (6.25-25 μM；作用 24 h) 可诱导 SW480 和 SW620 细胞发生 G2/M 期阻滞，该效应与 FOXM1 表达下调相关[1]。
FOXM1-IN-3 (6.25-25 μM；作用 24 小时) 在 12.5 μM 和 25 μM 浓度下可诱导 SW480 和 SW620 细胞发生凋亡[1]。
FOXM1-IN-3 (10 μM；24 h、48 h) 以 10 μM 浓度选择性靶向 SW480 和 SW620 细胞中的癌症干细胞 (CSC) 表型，对正常 CCD841 细胞仅产生轻微且可逆的作用[1]。
FOXM1-IN-3 具有高被动渗透性、低 CYP 干扰、显著的肝毒性 (HepG2 细胞中 IC50 ~5.6 μM) 和较低的神经毒性 (SH-SY5Y 细胞中 IC50 ~17 μM)[1]。

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

FOXM1-IN-3 相关抗体:

Cell Viability Assay[1]

Cell Line: SW620, SW480, CCD841
Concentration: 100 μM, 50 μM, 25 μM, 12.5 μM, 6.25 μM
Incubation Time: 24 h
Result: Demonstrated antiproliferative effects with IC₅₀ values of 14.9 μM (SW620), 17.5 μM (SW480), and 36.7 μM (CCD841), yielding selectivity indices of 2.1-2.5.

Cell Migration Assay[1]

Cell Line: SW480, SW620
Concentration: 25 μM, 12.5 μM, 6.25 μM
Incubation Time: 48 h
Result: Significantly impaired migration ability, with inhibition observed at 6.25 μM in SW480 cells and at 12.5 μM in SW620 cells.

Cell Cycle Analysis[1]

Cell Line: SW480, SW620
Concentration: 25 μM, 12.5 μM, 6.25 μM
Incubation Time: 24 h
Result: Induced a dose-dependent accumulation of cells in the G2/M phase along with a significant reduction in the S phase population in both cell lines.

Apoptosis Analysis[1]

Cell Line: SW480, SW620
Concentration: 25 μM, 12.5 μM, 6.25 μM
Incubation Time: 24 h
Result: Increased levels of both early and late apoptotic cells in a dose-dependent manner, particularly at 12.5 μM and 25 μM.
体内研究
(In Vivo)

FOXM1-IN-3 (compound 14) (5-10 μM；浸泡处理；72 小时) 可抑制斑马鱼结直肠癌异种移植模型中的肿瘤生长，其中对 SW620 细胞系的作用最为显著 (10 μM 剂量下肿瘤生长率为对照组的 80.95%)[1]。

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

Animal Model: Zebrafish species Danio rerio (wild-type AB)[1]
Dosage: 5, 10 μM
Administration: immersion; 72 hours
Result: For SW620 xenografts, showed 85.06% tumor growth relative to control at 5 μM and 80.95% at 10 μM at 3 days post-injection (dpi).
For SW480 xenografts, showed 92.65% tumor growth relative to control at 5 μM and 90.05% at 10 μM at 3 dpi.
分子量

564.12

Formula

C29H38ClN9O
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

FOXM1-IN-3 相关分类

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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:

FOXM1-IN-3PI3KCDKApoptosisPhosphoinositide 3-kinaseCyclin dependent kinasecolorectal cancer cellsSW620 cellsFOXM1CCD841 cellsCDC25G2/M cell cycle arrestzebrafish xenograft modelPI3KγapoptosisCCNB1Inhibitorinhibitorinhibit

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