2. GPCR/G Protein Neuronal Signaling Cell Cycle/DNA Damage
  3. 5-HT Receptor DNA/RNA Synthesis
  4. FOXM1-IN-4 hydrochloride

FOXM1-IN-4 (compound36) hydrochloride 是一种 5-HT7 受体拮抗剂和 FOXM1 调节剂，其对 5-HT7 受体的 Ki 为 92 nM，对 5-HT1A、5-HT2A 和 5-HT6 受体具有高选择性。 FOXM1-IN-4 (hydrochloride) 可阻断 5-HT7 受体信号通路，降低总 FOXM1 蛋白及磷酸化 FOXM1 蛋白水平，并下调 cyclin B1 和 cdc25B 的表达。 FOXM1-IN-4 (hydrochloride) 可诱导细胞周期 G2/M 期阻滞，减少 G0/G1 期细胞比例，并抑制克隆形成能力。 FOXM1-IN-4 (hydrochloride) 可抑制癌细胞增殖，可用于三阴性乳腺癌的相关研究。

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FOXM1-IN-4 hydrochloride

FOXM1-IN-4 hydrochloride Chemical Structure

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FOXM1-IN-4 hydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FOXM1-IN-4 (compound36) hydrochloride acts as a 5-HT7 receptor antagonist and FOXM1 modulator, with a Ki of 92 nM against the 5-HT7 receptor and high selectivity over 5-HT1A, 5-HT2A and 5-HT6 receptors. FOXM1-IN-4 (hydrochloride) blocks the 5-HT7 receptor signaling pathway, reduces the levels of total FOXM1 protein and phosphorylated FOXM1 protein, and downregulates the expression of cyclin B1 and cdc25B. FOXM1-IN-4 (hydrochloride) induces cell cycle arrest at the G2/M phase, decreases the proportion of cells in the G0/G1 phase, and inhibits clonogenic capacity. FOXM1-IN-4 (hydrochloride) suppresses cancer cell proliferation and is applicable to research related to triple-negative breast cancer[1].

体外研究
(In Vitro)

FOXM1-IN-4 (compound36) hydrochloride 可与 HEK293 细胞中表达的 5-HT7 受体结合，其 Ki 为 92 nM，Kb 为 11 nM[1]。
FOXM1-IN-4 (compound36) hydrochloride (孵育 24 h) 可抑制 MDA-MB-468、MDA-MB-231 和 Hs578T 三阴性乳腺癌细胞以及 NHDF 正常成纤维细胞的增殖，其 IC50 值分别为 7.1 μM、11.3 μM、6.7 μM 和 12.2 μM[1]。
FOXM1-IN-4 (compound36) hydrochloride (0.7-6.7 μM; 7 days) 可剂量依赖性地降低 MDA-MB-231 和 Hs578T 三阴性乳腺癌细胞的长期克隆形成存活率[1]。
FOXM1-IN-4 (hydrochloride) (1.5×IC50; 24 h) 可在 MDA-MB-231 三阴性乳腺癌细胞中诱导轻度 G2/M 期阻滞，并降低 G0/G1 期细胞比例，而在 Hs578T 细胞中无显著细胞周期影响[1]。
FOXM1-IN-4 (compound36) hydrochloride (1.5×IC50; 24 h) 可抑制 MDA-MB-231 三阴性乳腺癌细胞中 FOXM1、p-FOXM1 及 cyclin B1 的蛋白表达，同时上调 Hs578T 细胞中上述蛋白的表达水平[1]。
FOXM1-IN-4 (compound36) hydrochloride (0.5x IC50-2x IC50; 24 h) 可呈浓度依赖性抑制 MDA-MB-231 三阴性乳腺癌细胞的增殖；若在给予该化合物处理前，先用 10 μM 或 20 μM 血清素预处理细胞 48 h，其功效会进一步增强[1]。

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

FOXM1-IN-4 hydrochloride 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, Hs578T (triple-negative breast cancer cells)
Concentration: 0.7-5.7 μM (MDA-MB-231 cells); 0.8-6.7 μM (Hs578T cells)
Incubation Time: 7 days
Result: Significantly reduced colony numbers in MDA-MB-231 cells in a dose-dependent manner, with the strongest inhibition at 5.7 μM.
Significantly reduced colony numbers in Hs578T cells in a dose-dependent manner, with the strongest inhibition at 6.7 μM (equivalent to 0.5x IC50).

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231, Hs578T (triple-negative breast cancer cells)
Concentration: 1.5x IC50
Incubation Time: 24 h
Result: Caused a modest increase in the proportion of MDA-MB-231 cells in the G2/M phase and a marked decrease in the G0/G1 phase population.
Did not induce significant cell cycle arrest in Hs578T cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-231, Hs578T (triple-negative breast cancer cells)
Concentration: 1.5x IC50
Incubation Time: 24 h
Result: Reduced total FOXM1 levels by over 2.6-fold, reduced p-FOXM1 levels by approximately 2.7-fold, and reduced cyclin B1 expression in MDA-MB-231 cells; no significant reduction of cdc25B levels was observed relative to other compounds.
Increased FOXM1, p-FOXM1, cyclin B1, and cdc25B protein levels by >1.5-fold in Hs578T cells.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 (triple-negative breast cancer cells, serotonin-pretreated)
Concentration: 0.5x IC50-2x IC50 (compound); 10-20 μM (serotonin pretreatment)
Incubation Time: 24 h (compound treatment); 48 h (serotonin pretreatment)
Result: Inhibited cell proliferation in a concentration-dependent manner, with enhanced antiproliferative efficacy following pretreatment with 10 μM or 20 μM serotonin; the maximum effect was observed with 20 μM serotonin pretreatment.
分子量

493.05

Formula

C26H33ClN8
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-4 hydrochloride 相关分类

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  • 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-45-HT ReceptorDNA/RNA SynthesisSerotonin Receptor5-hydroxytryptamine Receptor5-HT7 receptornormal human dermal fibroblastscyclin B1cdc25BFOXM1HEK293 cells5-HT2A5-HT1A5-HT6 receptorstriple-negative breast cancer cell linesInhibitorinhibitorinhibit

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