VMY-1-101
VMY-1-101 is a fluorescent cyclin-dependent kinase (CDK) inhibitor, with an excitation of 410 nm and emission of 512 nm. VMY-1-101 competitively inhibits ATP binding to CDKs. VMY-1-101 induces G2/M cell cycle arrest in human breast cancer cells. VMY-1-101 induces modest apoptosis in human breast cancer cells. VMY-1-101 blocks proliferation of human breast cancer cells, including multidrug resistance-positive cells, and is not a substrate for p-glycoprotein. VMY-1-101 localizes to the cytoplasm of human breast cancer cells. VMY-1-101 shows increased binding to human breast cancer tissue compared to fluorophore alone. VMY-1-101 can be used for the research of breast cancer.
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- CAS No.: 1209002-42-5
- Formule: C33H40ClN9O4S
- Masse moléculaire:694.25
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
19.05 μM
Compound: VMY-1-101
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Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 48 hrs by WST-1 assay
Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 48 hrs by WST-1 assay
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[PMID: 21440449] |
In Vitro
VMY-1-101 (0.1 μM; 40 min) most potently inhibits the CDK2/cyclin E complex (87% inhibition) among tested purified human CDK/cyclin complexes, with varying degrees of inhibition across other CDK isoforms[1].
VMY-1-101 (1-100 μM; 48 h) potently inhibits the proliferation of human MDA-MB-231 breast cancer cells (IC50 = 4.86 μM) and MCF-7 breast cancer cells (IC50 = 19.05 μM) in a 48-h WST-1 assay[1].
VMY-1-101 (5-10 μM; 16 h, 24 h, 40 h) induces G2/M phase cell cycle arrest and moderate cell death in human MDA-MB-231 and MCF-7 breast cancer cells after 16 h, 24 h, or 40 h of treatment[1].
VMY-1-101 (10 μM; 48 h) reduces cell density and induces aberrant morphological changes in human MDA-MB-231 and MCF-7 breast cancer cells[1].
VMY-1-101 (10 μM; 48 h, 72 h) induces apoptotic signaling in human MDA-MB-231 breast cancer cells by altering Bcl-2/Bax protein levels and promoting PARP cleavage[1].
VMY-1-101 (10 μM; 24 h) induces significant early and late apoptosis in human MCF-7 breast 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:human MDA-MB-231 breast cancer cells, human MCF-7 breast cancer cells
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Concentration:5 μM; 10 μM
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Incubation Time:16 h, 24 h, 40 h
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Result:Induced a clear accumulation of cells in the G2/M phase in both MDA-MB-231 and MCF-7 cells at both 5 μM and 10 μM after 24 h.
Induced similar G2/M phase accumulation patterns at 16 h and 40 h.
Detected a moderate increase in sub-G1 cells (indicating cell death).
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Cell Line:human MDA-MB-231 breast cancer cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Reduced the level of anti-apoptotic Bcl-2 protein after 48 h of treatment.
Increased the level of pro-apoptotic Bax protein after 48 h of treatment, shifting the balance toward apoptosis.
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Cell Line:human MDA-MB-231 breast cancer cells
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Concentration:10 μM; 20 μM; 40 μM
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Incubation Time:72 h
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Result:Promoted moderate cleavage of the 116 kDa full-length PARP protein into an 89 kDa fragment, a marker of apoptotic signaling, after 72 h of treatment.
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Cell Line:human MCF-7 breast cancer cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Provoked a significant induction of early and late apoptotic cells, as indicated by increased annexin V-positive staining, relative to control cells.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 1209002-42-5
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Masse moléculaire 694.25
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Formule C33H40ClN9O4S
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SMILES
CC(C)N1C2=NC(N[C@@H](CO)CC)=NC(NC3=CC(Cl)=C(C=C3)C(NCCNS(=O)(C4=CC=CC5=C4C=CC=C5N(C)C)=O)=O)=C2N=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VMY-1-101 Related Classifications
HY-182383 Related Classifications
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