Chemical Name: 2-(1,1-Dimethylethyl)-9-fluoro-1,6-dihydro-7H-benz[h]imidazo[4,5-f]isoquinolin-7-one
Biological ActivityPotent pan-JAK inhibitor; ATP-competitive inhibitor of JAK 1/2/3 and Tyk2 (IC50 values are 1, 5, 15 and 1 nM, respectively). Inhibits other kinases tested at 130 nM to >10 μM. Inhibits IL-2- and IL-4-dependent proliferation of CTLL cells and blocks STAT5 phosphorylation. Also inhibits Th1 and Th2 development, and promotes Th17 differentiation from naive T cells. When used in combination with Retinoic acid, LY 294002 and CCG 1423, it induces intermediate mesoderm differentiation from ESCs. Inhibits growth of primary myeloma cells grown in the presence of bone marrow stromal cells. Cell-permeable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Combination of small molecules enhances differentiation of mouse embryonic stem cells into intermediate mesoderm through BMP7-positive cells.
Mae et al.
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.
Thompson et al.
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