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JAK3 Inhibitor C화학적 특성, 용도, 생산
개요
WHI-P154 is a quinazoline derivative that exhibits immunosuppressive effects by selectively inhibiting JAK3 (IC50 = 1.8 μM versus IC50s > 10 μM for JAK1 and JAK2). It has been reported to inhibit additional kinases including EGFR (IC50 = 4 nM) and VEGFR as well as the non-receptor tyrosine kinases, Abl, Lck, and Src. WHI-P154 is cytotoxic to human glioblastoma cells (IC50 = 813 nM) and has been used to induce the differentiation of neuronal precursor cells.
용도
WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM and also inhibits EGFR with IC50 of 4 nM.
Biochem/physiol Actions
WHI-P154 is a specific inhibitor of JAK3 (IC50 = 1.8 μM) with no inhibitory activity against JAK1 or JAK2. WHI-P154 enhances myogenic differentiation of C2C12 mouse myoblast cells, and induces differentiation of neural progenitor cells. The compound WHI-P154 dose dependently inhibits expression of iNOS and NO production in LPS-challenged macrophages.
