General Description
A cell-permeable, ATP competitive, and reversible indoloazepine compound that displays anti-proliferative and anti-inflammatory properties. Acts as a potent inhibitor of Chk2 (IC50 = 8 nM) that targets the ATP binding pocket. Exhibits selectivity for Chk2 over MEK1, Chk1, CK1δ, PKCα, PKCβII and CK2 (IC50 = 89 nM, 237 nM, 1.352 μM, 2.539 μM, 3.381 μM, and >10.0 μM, respectively). Blocks the production of IL-2 and TNF-α by preventing the transcriptional activation of NF-κB (IC50 = 3.55 μM for IL-2 production in PMA-stimulated Jurkat T cells; 8.16 μM for TNF-α production in LPS-stimulated THP-1 cells). Also reported to suppress the growth of leukemic T cells (GI50 = 1.73 μM).
