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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
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $48 | In Stock | |
5 mg | $118 | In Stock | |
10 mg | $188 | In Stock | |
25 mg | $358 | In Stock | |
50 mg | $548 | In Stock | |
100 mg | $738 | In Stock | |
200 mg | $993 | In Stock | |
1 mL x 10 mM (in DMSO) | $109 | In Stock |
Description | 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 |
In vitro | 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. |
Molecular Weight | 273.35 |
Formula | C15H15NO2S |
Cas No. | 113760-29-5 |
Smiles | CC1(C)Cc2oc(=Nc3ccccc3)sc2C(=O)C1 |
Relative Density. | 1.27 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (109.75 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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