Preferred Label : Emavusertib;
NCIt synonyms : Interleukin-1 Receptor-associated Kinase 4 Inhibitor CA-4948; IRAK4 Inhibitor CA-4948;
NCIt definition : An orally bioavailable, reversible inhibitor of interleukin-1 receptor-associated
kinase 4 (IRAK4), with potential antineoplastic, immunomodulating and anti-inflammatory
activities. Upon oral administration, emavusertib targets, binds to, and blocks the
kinase activity of IRAK4. This inhibits IRAK4-mediated signaling, prevents the activation
of IRAK4-mediated nuclear factor-kappa B (NF-kB) signaling and decreases the expression
of inflammatory cytokines and certain pro-survival factors. This inhibits proliferation
of IRAK4-overactivated tumor cells, which are found in cells harboring MYD88 activating
mutations or those with overactivated toll-like receptor (TLR) pathways. In addition,
CA-4948 may inhibit inflammation and immune-mediated cell destruction in inflammatory
and auto-immune diseases where TLR or interleukin 1 receptor (IL-1R) signaling is
overactivated and MYD88 is dysregulated. IRAK4, a serine/threonine-protein kinase
that plays a key role in both the TLR and IL-1R signaling pathways, is activated though
the adaptor protein MYD88 and links the TLR and IL-1R signaling pathway to the NF-kB
pathway.;
UNII : MH5DMF9JKY;
CAS number : 1801343-74-7;
Molecule name : CA-4948; AU 4948; CA 4948; AU-4948;
NCI Metathesaurus CUI : CL551081;
Origin ID : C148455;
UMLS CUI : C5554544;
Semantic type(s)
- concept_is_in_subset
- has_salt_form
- has_target
- is_free_acid_or_base_form_of
