Preferred Label : Selonsertib;
NCIt definition : An orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with
potential anti-inflammatory, antineoplastic and anti-fibrotic activities. Upon oral
administration, selonsertib targets and binds to the catalytic kinase domain of ASK1
in an ATP-competitive manner, thereby preventing its phosphorylation and activation.
This prevents the phosphorylation of downstream kinases, such as c-Jun N-terminal
kinases (JNKs) and p38 mitogen-activated protein kinase (p38 MAPK). By preventing
the activation of ASK1-dependent signal transduction pathways, GS-4997 prevents the
production of inflammatory cytokines, down-regulates the expression of genes involved
in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation. ASK1,
also called mitogen-activated protein kinase kinase kinase 5 (MAP3K5), is activated
in response to oxidative and endoplasmic reticulum (ER) stress, calcium influx and
infection. It plays a key role in the development of certain cardiovascular and neurodegenerative
diseases, diabetes, as well as certain types of cancer.;
UNII : NS3988A2TC;
InChIKey : YIDDLAAKOYYGJG-UHFFFAOYSA-N;
CAS number : 1448428-04-3;
Molecule name : GS-4997;
Origin ID : C121943;
UMLS CUI : C4724810;
Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
