EphB4-IN-2

EphB4-IN-2 (compound 66) is a tyrosine kinase inhibitor with an IC₅₀ value of 1.6 nM against human EphB4, and exhibits selectivity toward kinases bearing threonine gatekeeper residues. EphB4-IN-2 also has high ligand efficiency^[1]. In Vitro:EphB4-IN-2 (compound 66) (10 pM-20 μM; 2 h) potently inhibits recombinant EphB4 kinase activity with an IC₅₀ of 5 nM in a FRET-based enzymatic assay^[1].
EphB4-IN-2 (110 pM-10 μM; 30 minutes) inhibits recombinant EphB4 kinase activity with an IC₅₀ of 1.6 nM in a [γ-³³P]ATP-based enzymatic assay^[1].
EphB4-IN-2 (110 pM-10 μM; 30 minutes) potently inhibits 9 of 10 tested recombinant Eph receptor kinases with low nanomolar IC₅₀ values (1.1-15 nM), but shows reduced potency against EphA7 with an IC₅₀ of 1118 nM^[1].
EphB4-IN-2 (1 μM; 30 minutes) strongly inhibits recombinant EphA2, EphB3, Src, Lck, and Yes1 kinases, with intermediate activity against CSK, BTK, and HER-4, and minimal activity against most other tested kinases^[1].
EphB4-IN-2 (1 μM) binds with high affinity to 15 of 49 tested recombinant kinases with small gatekeeper residues, primarily in the Eph, Src, and Abl families^[1].