HG-9-91-01 is effective against a range of protein tyrosine kinases featuring a threonine residue at the gatekeeper position, including Src family kinases (Src, Lck, Yes), BTK, and receptors for FGF and Ephrin[1]. HG-9-91-01 can potentiate IL-10 production in bone marrow-derived dendritic cells (BMDCs) when pre-treated with zymosan, showing an EC50 of ~200 nM, an effect comparable to that induced by PGE2, suggesting a strong link between SIK2 inhibition and enhanced IL-10 production[2]. HG-9-91-01 exhibits significant selectivity for SIKs over AMPK in cell-free assays, with an over 100-fold higher potency against SIKs (IC50 against AMPK = 4.5 μM). Treatment with HG-9-91-01 dose-dependently increases mRNA expression of Pck1 and G6pc and glucose production[3].
体外研究
HG-9-91-01 is effective against a range of protein tyrosine kinases featuring a threonine residue at the gatekeeper position, including Src family kinases (Src, Lck, Yes), BTK, and receptors for FGF and Ephrin[1].
HG-9-91-01 can potentiate IL-10 production in bone marrow-derived dendritic cells (BMDCs) when pre-treated with zymosan, showing an EC50 of ~200 nM, an effect comparable to that induced by PGE2, suggesting a strong link between SIK2 inhibition and enhanced IL-10 production[2].
HG-9-91-01 exhibits significant selectivity for SIKs over AMPK in cell-free assays, with an over 100-fold higher potency against SIKs (IC50 against AMPK = 4.5 μM). Treatment with HG-9-91-01 dose-dependently increases mRNA expression of Pck1 and G6pc and glucose production[3].
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