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

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.

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Anticancer agent 304

Anticancer agent 304 Chemical Structure

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Anticancer agent 304 Related Antibodies

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Description

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].

In Vitro

Anticancer agent 304 (Compound 17) potently inhibits the proliferation of HepG2, Huh-7 and SK-Hep-1 cells, with IC50 values of 1.5 μM, 1.1 μM and 1.1 μM, respectively[1].
Anticancer agent 304 (0.5-1.5 μM; 24 h) inhibits clonogenic proliferation of SK-Hep-1 and Huh-7 cells, reduces the expression level of CDC45 protein in cells, and promotes nuclear export of CDC45 in cells[1].
Anticancer agent 304 (1.56-250 μM) binds directly to purified CDC45 protein, with a Kd of 83.0 μM[1].
Anticancer agent 304 (0.5-1.5 μM; 12 h) arrests SK-Hep-1 and Huh-7 cells at the G2/M phase of the cell cycle by upregulating p27 and downregulating p-CDC2[1].
Anticancer agent 304 (0.5-1.5 μM; 48 h) induces apoptosis in SK-Hep-1 and Huh-7 hepatocellular carcinoma cells by upregulating C-PARP-1 and downregulating PARP-1 and BCL-2[1].
Anticancer agent 304 (0.5-1.5 μM; 48 h) reverses epithelial-mesenchymal transition by upregulating E-cadherin and downregulating N-cadherin and Vimentin, and inhibits the migration and invasion of SK-Hep-1 and Huh-7 hepatocellular carcinoma cells[1].

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

Anticancer agent 304 Related Antibodies

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.
In Vivo

Anticancer agent 304 (30-60 mg/kg; i.p.; daily; 51 days) exhibits highly potent and non-toxic anti-hepatocellular carcinoma activity in hepatocellular carcinoma xenograft nude mice, achieving tumor weight inhibition rates of 76% and 84% at doses of 30 mg/kg and 60 mg/kg, respectively, while reducing the expression of CDC45 in tumor tissues[1].

MedChemExpress (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.
Molecular Weight

678.81

Formula

C42H46O8
SMILES

C[C@@]1(O)C2=C([C@]3(C)C[C@H]2C[C@H]3C(C4=CC=C(C([C@H]5[C@](C[C@H]6C5)(C)C7=C6[C@@](C)(O)CC[C@@H](C8=C)[C@@H]7OC8=O)=O)C=C4)=O)[C@@H]9[C@H](C(C(O9)=O)=C)CC1
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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:

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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