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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 | Availability | Quantity |
---|---|---|---|
25 mg | $2,420 | 10-14 weeks | |
50 mg | $3,180 | 10-14 weeks | |
100 mg | $4,300 | 10-14 weeks |
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 |
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. |
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