STAT5

9μM(EC₅₀,inK562cells)

STAT5

5μM(EC₅₀,inKU812cells)

STAT5-IN-2 is a STAT5 inhibitor, extracted from reference 1, example 17f. STAT5-IN-2 has potent antileukemic effect[1].

STAT5-IN-2 has EC50 values of 9 μM and 5 μM in K562 and KU812 cells, respectively[1].STAT5-IN-2 (100 nM-50 µM; 48 hours) has EC50 values of 2.6 µM and 3.5 µM in KG1a and MV-4-11 cells, respectively[1].STAT5-IN-2 (10 µM; 48 hours) induces apoptosis in all cell lines (K562, KU812, KG1a and MV-4-11 cells)[1]. STAT5-IN-2 (10 µM; 24 hours) blocks phosphorylation of STAT5[1].

[1]. Ludovic Juen, et al. New Inhibitor Targeting Signal Transducer and Activator of Transcription 5 (STAT5) Signaling in Myeloid Leukemias. J Med Chem. 2017 Jul 27;60(14):6119-6136.