Biological Activity
Proliferating cell nuclear antigen (PCNA) inhibitor. Directly binds PCNA trimers (Kd = 0.41 μM), reduces chromatin-associated PCNA in cells, inhibits cell growth through induction of S and G2M arrest, and attenuates DNA replication in cells. Inhibits growth of a range of tumor cell lines in vitro with IC50 values in the nanomolar to low micromolar range. Inhibits growth of prostate tumor xenografts in mice.
Technical Data
| M. Wt | 310.37 |
| Formula | C17H14N2O2S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 444930-42-1 |
| PubChem ID | 5410824 |
| InChI Key | WNYIQPCMVYAJLQ-JLHYYAGUSA-N |
| Smiles | O=C(C1=C(C)C=CS1)N/N=C/C2=C(O)C3=CC=CC=C3C=C2 |
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 | 31.04 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 310.37. 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 | 3.22 mL | 16.11 mL | 32.22 mL |
| 5 mM | 0.64 mL | 3.22 mL | 6.44 mL |
| 10 mM | 0.32 mL | 1.61 mL | 3.22 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Tan et al (2012) Small-molecule targeting of proliferating cell nuclear antigen chromatin association inhibits tumor cell growth. Mol.Pharmacol. 81 811 PMID: 22399488
Dillehay et al (2014) Antitumor effects of a novel small molecule targeting PCNA chromatin association in prostate cancer. Mol.Cancer Ther. 13 2817 PMID: 25253786
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