2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. PARP Bcl-2 Family Apoptosis
  4. Anticancer agent 304

Anticancer agent 304 是一种抗癌剂。Anticancer agent 304 结合 CDC45，Kd 为 83.0 μM。Anticancer agent 304 可将肝癌细胞周期阻滞于 G2/M 期，通过上调 C-PARP-1、下调 PARP-1 和 BCL-2 诱导细胞凋亡 (Apoptosis)，并抑制肝癌细胞的迁移、侵袭和增殖。Anticancer agent 304 在肝细胞癌动物模型中可抑制肿瘤生长。Anticancer agent 304 可用于肝癌的相关研究。

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Anticancer agent 304

Anticancer agent 304 Chemical Structure

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Anticancer agent 304 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anticancer agent 304 is an anticancer agent. Anticancer agent 304 binds to CDC45 with a Kd value of 83.0 μM. Anticancer agent 304 arrests the cell cycle of liver cancer cells at the G2/M phase, induces Apoptosis by upregulating C-PARP-1 and downregulating PARP-1 and BCL-2, and inhibits the migration, invasion and proliferation of liver cancer cells. Anticancer agent 304 suppresses tumor growth in animal models of hepatocellular carcinoma. Anticancer agent 304 is applicable to research related to liver cancer[1].

体外研究
(In Vitro)

Anticancer agent 304 (Compound 17) 可强效抑制 HepG2、Huh-7 和 SK-Hep-1 细胞的增殖，IC50 值分别为 1.5 μM、1.1 μM 和 1.1 μM[1]。
Anticancer agent 304 (0.5-1.5 μM; 24 h) 可抑制 SK-Hep-1 和 Huh-7 细胞的克隆形成增殖，降低细胞中的 CDC45 蛋白表达水平，促进细胞中 CDC45 的核输出[1]。
Anticancer agent 304 (1.56-250 μM) 可直接与纯化的 CDC45 蛋白结合，Kd 为 83.0 μM[1]。
Anticancer agent 304 (0.5-1.5 μM; 12 h) 可通过上调 p27 并下调 p-CDC2 将 SK-Hep-1 和 Huh-7 细胞阻滞于细胞周期的 G2/M 期[1] 。
Anticancer agent 304 (0.5-1.5 μM; 48 h) 可通过上调 C-PARP-1、下调 PARP-1 和 BCL-2，诱导 SK-Hep-1 和 Huh-7 肝癌细胞发生凋亡[1]。
Anticancer agent 304 (0.5-1.5 μM; 48 h) 可通过上调 E-cadherin、下调 N-cadherin 和 Vimentin 来逆转上皮间质转化，抑制 SK-Hep-1 和 Huh-7 肝癌细胞的迁移与侵袭[1]。

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

Anticancer agent 304 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Huh-7, SK-Hep-1 hepatocellular carcinoma cell lines
Concentration: 0 μM, 0.5 μM, 1.0 μM, 1.5 μM
Incubation Time: 24 h (initial treatment)
Result: Inhibited colony formation by 34.0% (0.5 μM), 72.9% (1.0 μM), and 97.6% (1.5 μM) in SK-Hep-1 cells.
Inhibited colony formation by 41.0% (0.5 μM), 64.7% (1.0 μM), and 89.1% (1.5 μM) in Huh-7 cells.

Western Blot Analysis[1]

Cell Line: Huh-7, SK-Hep-1 hepatocellular carcinoma cell lines
Concentration: 0 μM, 0.5 μM, 1.0 μM, 1.5 μM
Incubation Time: 24 h
Result: Significantly decreased CDC45 protein levels in both Huh-7 and SK-Hep-1 cells.

Cell Cycle Analysis[1]

Cell Line: Huh-7, SK-Hep-1 hepatocellular carcinoma cell lines
Concentration: 0 μM, 0.5 μM, 1.0 μM, 1.5 μM
Incubation Time: 12 h
Result: Arrested the cell cycle at the G2/M phase: in SK-Hep-1 cells, the percentage of G2/M phase cells increased from 23.5% to 27.1% (0.5 μM), 41.1% (1.0 μM), and 63.5% (1.5 μM); in Huh-7 cells, the percentage increased from 21.6% to 25.9% (0.5 μM), 28.2% (1.0 μM), and 34.8% (1.5 μM).
Upregulated p27 and downregulated p-CDC2 in both cell lines.

Immunofluorescence[1]

Cell Line: Huh-7, SK-Hep-1 hepatocellular carcinoma cell lines
Concentration: 0 μM, 0.5 μM, 1.0 μM, 1.5 μM
Incubation Time: 24 h
Result: Induced nuclear export of CDC45, decreasing nuclear localization and increasing cytoplasmic accumulation in both cell lines.

Apoptosis Analysis[1]

Cell Line: Huh-7, SK-Hep-1 hepatocellular carcinoma cell lines
Concentration: 0 μM, 0.5 μM, 1.0 μM, 1.5 μM
Incubation Time: 48 h
Result: Significantly induced apoptosis: in Huh-7 cells, the proportion of apoptotic cells increased from 4.8% to 14.4% (0.5 μM), 38.5% (1.0 μM), and 72.2% (1.5 μM); in SK-Hep-1 cells, the proportion increased from 2.1% to 28.7% (0.5 μM), 65.5% (1.0 μM), and 84.0% (1.5 μM).
Upregulated C-PARP-1 and downregulated PARP-1 and BCL-2 in both cell lines.
体内研究
(In Vivo)

Anticancer agent 304 (30-60 mg/kg; i.p.; every day; 51 days) 在肝细胞癌异种移植裸鼠中展现出高效且无毒的抗肝癌活性，在 30 mg/kg 和 60 mg/kg 剂量下分别实现 76%和 84%的肿瘤重量抑制率，同时可降低肿瘤组织中 CDC45 的表达[1]。

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

Animal Model: NU/NU nude mice (male, 4 weeks old, subcutaneously injected with Huh-7 cells)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: i.p.; every day; 51 days
Result: Inhibited tumor growth by 73% at 30 mg/kg after 51 days.
Reduced tumor weight by 76% at 30 mg/kg after 51 days.
Inhibited tumor growth by 84% at 60 mg/kg after 51 days.
Reduced tumor weight by 84% at 60 mg/kg after 51 days.
Reduced CDC45 protein expression in tumor tissues compared to controls.
Caused no compound-related body weight alterations.
Maintained serum levels of hepatic/renal biomarkers (ALT/GPT, AST/GOT, BUN, CRE) within normal ranges.
Showed no structural abnormalities in major organs (heart, liver, spleen, lung, kidney) via histopathological analysis.
分子量

678.81

Formula

C42H46O8
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

Anticancer agent 304 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:

Anticancer agent 304Anticancer agent304Anticancer agent-304PARPBcl-2 FamilyApoptosispoly ADP ribose polymerase anticancer agentHepG2 cellsHuh-7cellsSK-Hep-1 cellsNU/NU nude miceliver cancerInhibitorinhibitorinhibit

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