Preferred Label : ERK1/2 Inhibitor JSI-1187;
NCIt synonyms : ERK Inhibitor JSI-1187; Extracellular Signal-regulated Kinase 1/2 Inhibitor JSI-1187;
NCIt definition : An orally bioavailable inhibitor of the extracellular signal-regulated kinases 1 (ERK1)
and 2 (ERK2), with potential antineoplastic activity. Upon oral administration, ERK1/2
inhibitor JSI-1187 specifically targets, binds to and inhibits the activity of the
serine/threonine-protein kinases ERK1 and ERK2, thereby preventing the phosphorylation
of ERK1/2 substrates and the activation of mitogen-activated protein kinase (MAPK)/ERK-mediated
signal transduction pathways. This results in the inhibition of ERK-dependent proliferation
and survival of tumor cells. The MAPK/ERK pathway, also known as the RAS/RAF/MEK/ERK
pathway, is hyperactivated in a variety of tumor cell types due to mutations in upstream
targets. It plays a key role in the proliferation, differentiation and survival of
tumor cells.;
Molecule name : JSI-1187; JSI 1187;
NCI Metathesaurus CUI : CL1407830;
Origin ID : C174203;
UMLS CUI : C5418073;
- Semantic type(s)
- concept_is_in_subset
- has_target