Stemcell, 73552, WHI-P154

WHI-P154 is an inhibitor of Janus kinase 3 (JAK3) with IC₅₀ values of 28 and 128 μM against human and mouse proteins, respectively (Sudbeck et al.). It has also been reported to show significant inhibition of other kinases, including epidermal growth factor receptor (EGFR) in the nanomolar range (Changelian et al.; Uckun et al.). No significant inhibition of JAK1 or JAK2 has been observed (Sudbeck et al.).

DIFFERENTIATION

· Promotes differentiation of mouse neuronal precursor cells to neurons and oligodendrocytes, but blocks astrocyte differentiation (Kim et al.).

· Abolishes PDGF-induced increases in neurite outgrowth from human neural progenitor cells (Richards et al.).

IMMUNOLOGY

· Inhibits lipopolysaccharide (LPS)-induced nitric oxide synthase expression and nitric oxide production in macrophages and human epithelial cells (Sareila et al.).

CANCER RESEARCH

· Induces apoptosis and cell death in human glioblastoma cell lines U373 and U87. When coupled to EGF, inhibits tumor growth in mouse xenograft models (Narla et al.).