| Name | HI-TOPK-032 |
| Description | HI-TOPK-032 is an effective and specific inhibitor of TOPK. |
| In vitro | HI-TOPK-032 effectively suppresses both anchorage-dependent and independent growth of colon cancer cells by diminishing ERK-RSK phosphorylation and promoting apoptosis, evidenced by increased levels of p53, cleaved caspase-7, and cleaved PARP. At its highest concentration (5 μM), it also reduces MEK1 activity by 40%, showcasing its potency. While it significantly inhibits TOPK kinase activity, its impact on ERK1, c-jun-NH2-kinase 1, and p38 kinase activities remains minimal. The compound adeptly binds to the ATP-binding site of TOPK, forming hydrogen bonds with GLY83 and ASP151, and engaging in hydrophobic interactions with LYS30, highlighting its specificity and effective mechanism of action. |
| In vivo | HI-TOPK-032 (1 or 10 mg/kg; mice) treatment, obviously inhibits HCT-116 tumor growth by more than 60% relative to the vehicle-treated group. Mice are well tolerated with HI-TOPK-032 treatment. The expression of p53 is strongly caused, and phosphorylation of ERK and RSK, a direct downstream protein of ERK. Which is markedly inhibited in the HI-TOPK-032-treated group. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 3.7 mg/mL (10.02 mM), Sonication is recommended.
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| Keywords | TOPK | Inhibitor | inhibit | HI-TOPK-032 | HI-TOPK032 | HITOPK032 | HI-TOPK 032 | HI TOPK 032 |
| Inhibitors Related | Ilaprazole sodium hydrate | Ilaprazole | OTS964 | Cephradine | Cephradine (Standard) | Cephradine monohydrate | Cephradine sodium | OTS514 | OTS514 hydrochloride | Ilaprazole sodium | OTS964 hydrochloride |
| Related Compound Libraries | Reprogramming Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Cancer Compound Library | MAPK Inhibitor Library |
United States
