Preferred Label : Type II JAK2 Inhibitor AJ1-11095;
NCIt synonyms : JAK2 Inhibitor AJ1-11095;
NCIt definition : An orally bioavailable inhibitor of the type II conformation of Janus-associated kinase
2 (JAK2), with potential antineoplastic activity. Upon oral administration, type II
JAK2 inhibitor AJ1-11095 specifically targets and binds to the inactive, DFG-loop-out
conformation of the JAK2 domain, which stabilizes JAK2 in an inactive, DFG-loop-out
conformation, and blocks the ATP-binding site and the adjoining hydrophobic pocket.
This inhibits JAK2 activation, and thereby prevents the activation of the JAK/signal
transducer and activator of transcription (STAT) signaling pathway and the activation
of STAT3 and STAT5. This may lead to an induction of tumor cell apoptosis and a decrease
in tumor cell proliferation. JAK2, often upregulated or mutated in a variety of cancer
cells, mediates STAT3 activation and plays a key role in tumor cell proliferation
and survival.;
Molecule name : AJ1 11095; AJ1-11095;
Origin ID : C210745;
concept_is_in_subset
- has_target
