Biological Activity
T-LAK-cell-originated protein kinase (TOPK) inhibitor; exhibits selectivity for TOPK over other MAPKK family members including ERK1, JNK1 and p38. Blocks proliferation of HCT116 colon cancer cells; suppresses tumor growth in a colon cancer xenograft model. Also inhibits Chk1 (IC50 = 9.6 μM).
Technical Data
| M. Wt | 369.4 |
| Formula | C20H11N5OS |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 487020-03-1 |
| PubChem ID | 1936439 |
| InChI Key | BCSBXWKRZUPFHW-UHFFFAOYSA-N |
| Smiles | O=C(C5=CC=CS5)NC4=CC3=C(C#N)C2=NC1=CC=CC=C1N=C2N3C=C4 |
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 | 7.39 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 369.4. 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 | 2.71 mL | 13.54 mL | 27.07 mL |
| 5 mM | 0.54 mL | 2.71 mL | 5.41 mL |
| 10 mM | 0.27 mL | 1.35 mL | 2.71 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Li et al (2011) Discovery of novel checkpoint kinase 1 inhibitors by virtual screening based on multiple crystal structures. J.Chem.Inf.Model. 51 2904 PMID: 21955044
Kim et al (2012) Novel TOPK inhibitor HI-TOPK-032 effectively suppresses colon cancer growth. Cancer Res. 72 3060 PMID: 22523035
Keywords: HI TOPK 032, supplier, HITOPK032, TOPK, T-LAK-cell-originated, protein, kinase, MAPKK, inhibitors, inhibits, selective, antitumor, colon, cancer, cells, antiproliferatives, Other, MAPK, Other, MAPK, Tocris Bioscience
