[CAS NO. 1456858-58-4]  HG-9-91-01

HG-9-91-01 inhibits a number of protein tyrosine kinases that possess a threonine residue at the gatekeeper site, such as Src family members (Src, Lck, and Yes), BTK, and the FGF and Ephrin receptors ^[1] . HG-9-91-01 demonstrates a strong correlation between the potency of SIK2 inhibition and enhanced IL-10 production. In agreement with these reports, pretreating BMDCs with HG-9-91-01, a recently described inhibitor of SIK1-3, along with several other kinases, results in concentration-dependent potentiation of zymosan-induced IL-10 production with an EC ₅₀ ~200 nM and a maximum effect similar to that observed with PGE ₂ ^[2] . HG-9-91-01 has more than a 100-fold greater potency against SIKs than AMPK (IC ₅₀ =4.5 μM) in a cell-free assay. HG-9-91-01 treatment dose dependently increased mRNA expression of Pck1 and G6pc and that effect is similar in cells treated with 4 μM HG-9-91-01. Consistent with this observation, there is also a dose-dependent increase in glucose production following HG-9-91-01 treatment ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.