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 是一种可渗透细胞的苯并恶硫醇化合物。

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 compound

BOT-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.

113760-29-5

C15H15NO2S

273.35

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years