Type II JAK2 Inhibitor AJ1-11095

**Semantic type:** Pharmacologic Substance

**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.

**Synonyms:** - AJ1 11095 - AJ1-11095 - AJ111095 - JAK2 Inhibitor AJ1-11095