BOT-64

Research use only, not for human use.

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 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.

——

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

——

Immunology/Inflammation

IκB kinase (IKK)

IKK2

——

——

113760-29-5

273.35

C15H15NO2S

>98% (HPLC)

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

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

——

(-20℃)

With Ice Pack

≥ 2 years