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Cbl-b-IN-16 (compound 31) is an orally active inhibitor of the RING E3 ligase Cbl-b, with an IC50 of 30 nM. It enhances IL-2 production in human T cells with an EC50 of 230 nM and exhibits antitumor activity.
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| Description | Cbl-b-IN-16 (compound 31) is an orally active inhibitor of the RING E3 ligase Cbl-b, with an IC50 of 30 nM. It enhances IL-2 production in human T cells with an EC50 of 230 nM and exhibits antitumor activity. |
| In vitro | Cbl-b-IN-16 modulates the TCR signaling pathway by inhibiting Cbl-b ubiquitination and its transfer to Zap-70, with IC₅₀ values of 63 nM and 84 nM, respectively. At a concentration of 5 μM and an exposure time of 20 minutes, Cbl-b-IN-16 inhibits Cbl-b phosphorylation via SYK. This compound enhances the TCR signaling pathway by inhibiting effects, leading to an upregulation of pPLCγ1 levels in human T cells, with an EC₅₀ of 0.61 μM. |
| Formula | C26H27F3N6O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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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