Biological Activity
E2F transcription factor inhibitor; inhibits E2F DNA binding activity. Inhibits E2F4 DNA binding and reduces E2F4 protein levels in A375 melanoma cells. Induces apoptosis of A375 and MDA-MB-231 breast cancer cells. Inhibits A375 proliferation and invasion in a three dimensional skin model of A375 invasion. Also attenuates human embryonic stem cell proliferation.
Technical Data
| M. Wt | 399.48 |
| Formula | C25H25N3O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 353519-63-8 |
| PubChem ID | 2895500 |
| InChI Key | CYNZBLNMIJNBSF-UHFFFAOYSA-N |
| Smiles | CC1=C(OCC)C=CC(C(C3=C(O)C(N=C(C)C=C4)=C4C=C3)NC2=NC=CC=C2)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.99 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 399.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.5 mL | 12.52 mL | 25.03 mL |
| 5 mM | 0.5 mL | 2.5 mL | 5.01 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.5 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ma et al (2008) A small-molecule E2F inhibitor blocks growth in a melanoma culture model. Cancer Res. 68 6292 PMID: 18676853
Conklin et al (2012) The RB family is required for the self-renewal and survival of human embryonic stem cells. Nat.Commun. 3 1244 PMID: 23212373
Keywords: HLM 006474, supplier, HLM006474, E2F, transcription, factors, inhibits, inhibitors, DNA, binding, A375, melanoma, stems, cells, proliferation, human, embryonic, Other, Transcription, Factors, Stem, Cell, Proliferation, Other, Transcription, Factors, Tocris Bioscience
