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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $48 | In Stock | In Stock | |
| 5 mg | $118 | In Stock | In Stock | |
| 10 mg | $188 | In Stock | In Stock | |
| 25 mg | $358 | In Stock | In Stock | |
| 50 mg | $548 | In Stock | In Stock | |
| 100 mg | $738 | In Stock | In Stock | |
| 200 mg | $993 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $109 | In Stock | 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 |
| Targets&IC50 | IKKβ:1 μM |
| 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 | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 30 mg/mL (109.75 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.32 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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