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HG-12-6 is a type II inhibitor of IRAK4, demonstrating preferential binding to unphosphorylated inactive IRAK4 (IC50: 165 nM) and modulating IRAK4 activity in autoimmunity and inflammation.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $2,720 | 3-6 months | 3-6 months | |
| 50 mg | $3,580 | 3-6 months | 3-6 months | |
| 100 mg | $4,900 | 3-6 months | 3-6 months |
| Description | HG-12-6 is a type II inhibitor of IRAK4, demonstrating preferential binding to unphosphorylated inactive IRAK4 (IC50: 165 nM) and modulating IRAK4 activity in autoimmunity and inflammation. |
| Targets&IC50 | IRAK4:165 nM , IRAK4:2876 nM |
| In vitro | HG-12-6 has a better binding affinity for the unphosphorylated inactive IRAK4 kinase domain (IC50 of 165 nM) than the phosphorylated active IRAK4 kinase domain (IC50 of 2876 nM).The in-house compound HG-12-6 has a similar chemical scaffold as Ponatinib.?The most differentiating components are the head of the inhibitor and the lack of a methyl substituent on ring A. Without the methyl substituent on ring A, the entire HG-12-6 molecule shifts inward to the ATP pocket in comparison with the binding mode of Ponatinib. |
| Molecular Weight | 580.62 |
| Formula | C29H27F3N6O2S |
| Cas No. | 2222354-57-4 |
| Smiles | N(C(=O)C1CC1)C=2SC=3C(N2)=CC=C(N3)C4=CC(C(NC5=CC(C(F)(F)F)=C(CN6CCNCC6)C=C5)=O)=CC=C4 |
| Relative Density. | 1.444 g/cm3 (Predicted) |
| 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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