Pomstafib-2

Pomstafib-2 is a potent and selective STAT5b inhibitor. Pomstafib-2 decreases the expression of pSTAT5b and induces Apoptosis[1][2].

Signaling Pathways >> Stem Cell/Wnt >> STAT

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> STAT

Pomstafib-2 (compound 8) (0-10 µM; 4 h) decreases the expression of pSTAT5b in a dose-dependent manner in STAT5b-GFP-transfected K562 cells[1]. Pomstafib-2 (0, 10, 20, 40, 60, 80 µM; 48 h) induces apoptosis in a dose-dependent manner in STAT5-dependent K562 cells[1]. Western Blot Analysis[1] Cell Line: K562 leukaemia cells Concentration: 0, 0.3, 1, 3, 10 µM Incubation Time: 4 h Result: Decreased the expression of pSTAT5b in a dose-dependent manner. Apoptosis Analysis[1] Cell Line: K562, MDA-MB-231 cells Concentration: 0, 10, 20, 40, 60, 80 µM Incubation Time: 48 h Result: Induced apoptosis in a dose-dependent manner in K562 cells, does not increased the apoptotic rate of STAT5-independent MDA-MB-231 cells.

[1]. Elumalai N, et al. Rational development of Stafib-2: a selective, nanomolar inhibitor of the transcription factor STAT5b. Sci Rep. 2017 Apr 11;7(1):819.  

[2]. Gräb J, et al. The STAT5b Linker Domain Mediates the Selectivity of Catechol Bisphosphates for STAT5b over STAT5a. ACS Chem Biol. 2019 Apr 19;14(4):796-805.