Antitumor agent-226
Antitumor agent-226 is a DNMT3A inhibitor and epigenetic modulator. Antitumor agent-226 inhibits cell proliferation and migration by downregulating DNA Methyltransferase, reducing global DNA methylation, and modulating JNK, ERK1/2, and p38 phosphorylation through the MAPK pathway to induce mitochondria-dependent apoptosis, G2/M phase arrest, autophagy, and ROS production. Antitumor agent-226 can be used for research on prostate cancer.
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- CAS 番号: 3056235-77-6
- 分子式: C25H21ClF2N4O5
- 分子量:530.91
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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DNA Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
DNMT3A |
ERK1 |
ERK2 |
JNK |
p38 MAPK |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1.58 μM
|
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
|
42612263 |
| PC-3 | IC50 |
1.35 μM
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Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
|
42612263 |
| T47D | IC50 |
1.55 μM
|
Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
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42612263 |
| SMMC-7721 | IC50 |
1.79 μM
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Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
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42612263 |
| HEK293 | IC50 |
11.22 μM
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Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
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42612263 |
体外実験
Antitumor agent-226 (compound 11M) (0.625-10 μM; 48 h) exhibits the strongest antiproliferative activity against A549 and PC-3 cell lines, with IC50 values of 1.58 μM and 1.51 μM, respectively, and shows the highest selectivity index in PC-3 cells (SI = 8.31)[1].
Antitumor agent-226 (1-3 μM; 24 h) inhibits PC-3 cell proliferation in a dose-dependent manner and induces morphological changes characteristic of cell death[1].
Antitumor agent-226 (1-3 μM; 24 h) significantly inhibits the colony-forming ability of PC-3 cells[1].
Antitumor agent-226 (1-3 μM; 24-48 h) significantly inhibits the migration of PC-3 cells[1].
Antitumor agent-226 (1-3 μM) combined with Acetylcysteine (NAC) (HY-B0215) restores the viability of PC-3 cells[1].
Antitumor agent-226 (1-3 μM; 24 h) induces G2/M phase cell cycle arrest in PC-3 cells[1].
Antitumor agent-226 (1-3 μM; 24 h) induces G2/M phase arrest in PC-3 cells by upregulating p21 and downregulating Cyclin B1 and CDK1[1].
Antitumor agent-226 (1-3 μM; 24 h) induces apoptosis in PC-3 cells through downregulation of Bcl-2 and Bax[1].
Antitumor agent-226 (1-3 μM; 24 h) activates the MAPK signaling pathway in PC-3 cells by increasing the phosphorylation of JNK, ERK1/2, and p38[1].
Antitumor agent-226 (1-3 μM; 24 h) induces apoptotic nuclear morphological changes in PC-3 cells[1].
Antitumor agent-226 (1-3 μM; 24 h) induces apoptosis in PC-3 cells in a dose-dependent manner[1].
Antitumor agent-226 (1-3 μM) induces apoptosis in PC-3 cells, and inhibition of autophagy promotes this apoptotic effect[1].
Antitumor agent-226 (1-3 μM; 24 h) induces autophagy in PC-3 cells by increasing LC3-II expression and promoting the conversion of LC3-I to LC3-II[1].
Antitumor agent-226 (3 μM; 24 h) induces autophagy in PC-3 cells, manifested by the formation of autophagosomes[1].
Antitumor agent-226 (1-3 μM) increases the expression level of LC3-II in PC-3 cells; combined treatment with the autophagy inhibitor 3-Methyladenine (3-MA) (HY-19312) reverses this effect[1].
Antitumor agent-226 (1-3 μM; 24 h) significantly downregulates DNMT3A protein levels in PC-3 cells[1].
Antitumor agent-226 (3 μM; 24 h) significantly alters gene expression in PC-3 cells, particularly affecting metabolic processes, intracellular structures, and the MAPK signaling pathway[1].
Antitumor agent-226 (3 μM; 24 h) reduces global DNA methylation levels in PC-3 cells, leading to genome-wide hypomethylation[1].
Antitumor agent-226 (1-3 μM; 24 h) induces a dose-dependent decrease in mitochondrial membrane potential in PC-3 cells[1].
Antitumor agent-226 (1-3 μM; 24 h) induces ROS production in PC-3 cells[1].
Antitumor agent-226 (1-3 μM) modulates the expression of cell cycle regulatory proteins P21, CyclinB1, and CDK1 in prostate cancer cells[1].
Antitumor agent-226 (1-3 μM) alters the expression of apoptosis-related proteins Bax and Bcl-2 in prostate cancer cells[1].
Antitumor agent-226 (1-3 μM) affects the MAPK signaling pathway by modulating the phosphorylation of JNK, ERK, and P38 in prostate cancer cells[1].
Antitumor agent-226 (1-3 μM) induces autophagy in prostate cancer cells, manifested as modulation of LC3-I and LC3-II levels[1].
Antitumor agent-226 (1-3 μM) downregulates DNMT3A expression in prostate cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3
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Concentration:1, 1.5, 2, 2.5, 3 μM
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Incubation Time:24 h
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Result:Caused significant morphological changes including cell shrinkage, fragmentation, rounding, and detachment.
Decreased cell viability gradually with increasing concentrations.
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Cell Line:PC-3
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Concentration:1, 2, 3 μM
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Incubation Time:24 h
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Result:Induced a marked reduction in colony numbers compared to the untreated group.
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Cell Line:PC-3
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Concentration:1, 2, 3 μM
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Incubation Time:24, 48 h
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Result:Significantly inhibited PC-3 cell migration at 0, 24, and 48 h.
Strongly inhibited migration at concentrations of 2 μM and 3 μM.
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Cell Line:PC-3
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Concentration:1, 2, 3 μM
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Incubation Time:24 h
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Result:Increased the proportion of cells in G2/M phase to 19.7% at 1 μM.
Increased the proportion of cells in G2/M phase to 24.8% at 2 μM.
Increased the proportion of cells in G2/M phase to 27.4% at 3 μM.
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Cell Line:PC-3
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Concentration:1, 3 μM
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Incubation Time:24 h
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Result:Markedly upregulated the expression of p21.
Downregulated the expression of Cyclin B1 and CDK1.\nDownregulated the expression of apoptosis-related proteins Bcl-2 and Bax.\nSignificantly increased the phosphorylation levels of JNK, ERK1/2, and p38, while total protein levels remained unchanged.\nIncreased LC3-II expression.
Promoted the conversion of LC3-I to LC3-II.\nSignificantly reduced DNMT3A protein levels.
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Cell Line:PC-3
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Concentration:1, 2, 3 μM
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Incubation Time:24 h
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Result:Induced intense, concentrated blue fluorescence in nuclei, a hallmark of early apoptosis, which became more pronounced with increasing concentrations.
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Cell Line:PC-3
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Concentration:1, 2, 3 μM
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Incubation Time:24 h
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Result:Reduced mitochondrial membrane potential in 28.83% of cells at 1 μM.
Reduced mitochondrial membrane potential in 42.21% of cells at 2 μM.
Reduced mitochondrial membrane potential in 81.11% of cells at 3 μM.\nSignificantly increased ROS levels compared to the control group.
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Cell Line:PC-3
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Concentration:1, 2, 3 μM
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Incubation Time:24 h
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Result:Induced apoptosis rates of 8.49% at 1 μM.
Induced apoptosis rates of 35.43% at 2 μM.
Induced apoptosis rates of 38.99% at 3 μM.
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Cell Line:PC-3
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Concentration:3 μM
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Incubation Time:24 h
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Result:Revealed the presence of autophagic vacuoles and autophagosomes, suggesting active autophagy.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (male, 5 weeks old, subcutaneous PC-3 cell xenograft model)[1]
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Dosage:5 mg/kg
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Administration:i.p.; every two days; 21 days
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Result:Significantly reduced tumor volume and weight compared to control and cisplatin groups.
Induced extensive apoptosis and necrosis with nuclear fragmentation and cytoplasmic vacuolation.
Significantly increased apoptosis by TUNEL staining.
Significantly upregulated phosphorylated ERK (p-ERK) levels while total ERK expression remained stable.
Downregulated DNMT3A expression.
Showed no significant weight loss or signs of toxicity.
Showed no significant pathological changes in H&E-stained sections of the heart, liver, spleen, lungs, and kidneys.
- Cell migration
- Somatic Cell Culture
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Autophagy
- Apoptosis Solutions
- Lysosome and acidic-vesicle live-cell staining
- MTT Cell Proliferation Assay
- Macroautophagy Solutions
- Western Blot
- Research Protocol for Epigenomic Data Analysis
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- ROS/oxidative-stress fluorescent staining
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Protocol for Kinase activity and phosphorylation assays
化学情報
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CAS 番号 3056235-77-6
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分子量 530.91
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分子式 C25H21ClF2N4O5
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SMILES
O=C1C(Cl)=CCCN1C(/C=C/C2=CC=C(OCC3=CN(C4=CC=C(OC(F)F)C=C4)N=N3)C(OC)=C2)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Antitumor agent-226 関連分類
HY-189265 関連分類
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