HI-TOPK-032 is a potent and selective TOPK inhibitor. In vitro, HI-TOPK-032 strongly suppressed TOPK kinase activity but had little effect on extracellular signal–regulated kinase 1 (ERK1), c-jun—NH2—kinase 1, or p38 kinase activities. HI-TOPK-032 also inhibited anchorage-dependent and -independent colon cancer cell growth by reducing ERK-RSK phosphorylation as well as increasing colon cancer cell apoptosis through regulation of the abundance of p53, cleaved caspase-7, and cleaved PARP. In vivo, administration of HI-TOPK-032 suppressed tumor growth in a colon cancer xenograft model. HI-TOPK-032 may be further developed as a potential therapeutic against colorectal cancer. The serine-threonine mitogen-activated protein kinase kinase family member T-LAK cell–originated protein kinase (TOPK/PBK) is heavily involved in tumor development, cancer growth, apoptosis, and inflammation ( Cancer Res; 72(12); 3060–8.).
MedKoo Cat#: 407118
Name: HI-TOPK-032
CAS#: 487020-03-1
Chemical Formula: C20H11N5OS
Exact Mass: 369.0684
Molecular Weight: 369.20
Elemental Analysis: C, 65.03; H, 3.00; N, 18.96; O, 4.33; S, 8.68
The following data is based on the product molecular weight 369.20 Batch specific molecular weights may vary from batch to batch due to the degree 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 | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
