BOT-64

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BOT-64 是一种 IKK-2 抑制剂，靶向激酶激活环结构域中的 Ser177 和/或 Ser181 残基。BOT-64 是一种细胞可渗透的苯并氧硫醇化合物。BOT-64 抑制 LPS 激活的巨噬细胞中 IKKbeta 介导的 IkappaBα 磷酸化，从而产生顺序预防下游事件，包括 IkappaBalpha 的蛋白水解降解、DNA 结合能力和 NF-kappaB 的转录活性。

BOT-64 is an IKK-2 inhibitor which targets the Ser177 and/or Ser181 residues in the kinase's activation loop domain.BOT-64 is a cell-permeable benzoxathiole compoundBOT-64 inhibits IKKbeta-mediated IkappaBalpha phosphorylation in LPS-activated macrophages, resulting in sequential prevention of downstream events, including proteolytic degradation of IkappaBalpha, DNA binding ability, and transcriptional activity of NF-kappaB.?BOT-64 inhibits LPS-inducible IKKbeta activity in the cells and catalytic activity of highly purified IKKbeta.?Moreover, the effect of BOT-64 on cell-free IKKbeta was abolished by substitution of Ser-177 and Ser-181 residues in the activation loop of IKKbeta to glutamic acid residues, indicating a direct interaction site of benzoxathiole.?BOT-64 attenuates NF-kappaB-regulated expression of inflammatory genes such as inducible nitric-oxide synthase, cyclooxygenase-2, tumor necrosis factor-alpha, interleukin (IL)-1beta, and IL-6 in LPS-activated or expression vector IKKbeta-transfected macrophages.?

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BOT-64 (3-30 mg/kg) increases the survival rates of endotoxin LPS-shocked mice.

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Immunology/Inflammation

IκB kinase (IKK)

IKK2

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113760-29-5

273.35

C15H15NO2S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (365.83 mM)

CC1(C)Cc2oc(=Nc3ccccc3)sc2C(=O)C1

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(-20℃)

With Ice Pack

≥ 2 years