HG-12-6
CAS No. : 2222354-57-4
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| Cat. No. : | HY-123956 |
| M.Wt: | 580.62 |
| Formula: | C29H27F3N6O2S |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation[1].
In Vitro: 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[1].
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)[1].
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