Powder: -20°C for 3 years | In solvent: -80°C for 1 year
HI-TOPK-032 is an effective and specific inhibitor of TOPK.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
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2 mg | 在庫あり | ¥ 9,000 | |||
5 mg | 在庫あり | ¥ 14,500 | |||
10 mg | 在庫あり | ¥ 21,500 | |||
25 mg | 在庫あり | ¥ 45,500 | |||
50 mg | 在庫あり | ¥ 77,500 | |||
100 mg | 在庫あり | ¥ 133,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 16,000 |
説明 | 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. |
分子量 | 369.4 |
分子式 | C20H11N5OS |
CAS No. | 487020-03-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7 mg/mL (18.94 mM)
You can also refer to dose conversion for different animals. 詳細
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HI-TOPK-032 487020-03-1 MAPK TOPK HITOPK032 inhibit HI TOPK 032 HI-TOPK032 HI-TOPK 032 Inhibitor inhibitor