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化學性質:
規格 | 5mg 10mg 50mg |
CAS | 445430-58-0 |
別名 |
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化學名 |
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分子式 | C14H17N5 |
分子量 | 255.32 |
溶解度 | ≥ 70mg/mL in DMSO |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
BMS-345541(free base) is a selective inhibitor of IKK-1 and IKK-2 with IC50 value of 4μM and 0.3μM, respectively [1].
IKK is also known as nuclear factor kappa-B kinase subunit inhibitor and involves in cytokine-activated intracellular signaling pathways. IKK-1 and IKK-2 are members of IKK family. It has been reported that IKK-2 plays a pivotal role in brain cells following a stroke [2] [3].
BMS-345541 is a potent IKK inhibitor and has a highly selective activity compared with other kinases. When tested with THP-1 monocytic cells, pre-incubation with BMS-345541 inhibited TNF-α-stimulated IKK phosphorylation and reduced a variety of cytokines production including TNF-α, IL-1β, IL-8, and IL-6 [1]. In 4 human glioma cell lines, BMS-345541 treatment significantly blocked cell proliferation (80%-95%) at the concentration of 10 μM or higher and also inhibited IL-8 expression in a dose dependent manner (IC50>2 μM) [2]. And similar result of BMS-34551 inhibition on IKK which induced cell apoptosis was verified in human melanoma cell lines SK-MEL-5, Hs 294T, and A375 [3].
In 18-22g female BALB/c mice model, administration of BMS-345541 inhibited TNF-αproduction in a dose-dependent manner, ~50% inhibition was seen when used the concentration of 10 mg/kg and near complete inhibition was seen at a dose of 100 mg/kg [1].
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原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278