产品说明书
BMS-345541 HCl
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同义名 : | BMS 345541 (hydrochloride);IKK Inhibitor III;BMS-345541 hydrochloride |
| CAS号 : | 547757-23-3 | |
| 货号 : | A901193 | |
| 分子式 : | C14H18ClN5 | |
| 纯度 : | 99%+ | |
| 分子量 : | 291.779 | |
| MDL号 : | MFCD07784499 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 18 mg/mL(61.69 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 50 mg/mL(171.36 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | NF-κB normally exists in the cytoplasm of unstimulated cells as an inactive complex with a member of the IκB inhibitory protein family. This class of protein includes IκBα, IκBβ, and IκBε. IKK-1 and IKK-2 are two catalytic subunits of IκB kinase (IKK). BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively[3]. In vitro, BMS-345541 at 0, 0.1, 1, and 10 μM treatment resulted in a concentration-dependent inhibition of melanoma cell (SK-MEL-5, A375, and Hs 294T) proliferation[4]. In vivo, BMS-345541 (0, 10, 25, and 75 mg/kg) was administered to melanoma tumor-bearing mice orally once daily for 21 days, and it was showed that BMS-345541 effectively inhibited SK-MEL-5 tumor growth in a dose-dependent manner[4]. BMS-345541 also dose-dependently inhibited the production of TNFα in the serum of animals challenged with an intraperitoneal administration of LPS. Approximately 50% inhibition was observed at 10 mg/kg, and dose of 100 mg/kg nearly completely inhibit serum TNFα[3]. | ||
| 作用机制 | BMS-345541 binds to an allosteric site on IKK-2 and IKK-1. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.43mL 0.69mL 0.34mL |
17.14mL 3.43mL 1.71mL |
34.27mL 6.85mL 3.43mL |
| 参考文献 |
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