MS-1020

MS-1020 is a potent and ATP-competitive JAK3 inhibitor. MS-1020 inhibits JAK3/STAT signaling and induces apoptosis. MS-1020 promotes cell death. MS-1020 decreases the expression of tyrosine phosphorylated STAT3 levels. MS-1020 has the potential for the research of cancers harboring aberrant JAK3 signaling[1].

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> JAK

Signaling Pathways >> Epigenetics >> JAK

Signaling Pathways >> Stem Cell/Wnt >> JAK

JAK3

MS-1020 (0-50 µM; 24 h) inhibits STAT92E transcriptional activity in cultured Drosophila cells[1]. MS-1020 (0, 10, 30 , 50 µM) decreases the expression of tyrosine phosphorylated STAT3 levels and shows no changes on total STAT3 levels[1]. MS-1020 (0, 10, 30 , 50 µM; 16 h) decreases the expression of IL-2 (100 ng/ml)-induced STAT5 phosphorylation in Nb2 cells[1]. MS-1020 (0, 10, 30 , 50 µM; 72 h) promotes cell death in a time- and dose-dependent manner in L540 cells[1]. MS-1020 (0, 10, 30 , 50 µM; 72 h) induces apoptosis in L540 cells[1]. Western Blot Analysis[1] Cell Line: L540, HDLM-2, MDA-MB-468 cells Concentration: 0, 10, 30, 50 µM Incubation Time: Result: Decreased the expression of tyrosine phosphorylated STAT3 levels in a dose-dependent manner and showed no changes on total STAT3 levels. Cell Viability Assay[1] Cell Line: L540, HDLM-2 cells Concentration: 0, 10, 30, 50 µM Incubation Time: 72 h Result: Promoted cell death in a time- and dose-dependent manner only in L540 cells. Apoptosis Analysis[1] Cell Line: L540 cells Concentration: 0, 10, 30, 50 µM Incubation Time: 72 h Result: Induced apoptosis in L540 cells and increased the expression of cleavage of Poly (ADP-ribose) polymerase (PARP) and cleaved caspase-3 and cleaved caspase-3, decreased the expression of Bcl-2, Bcl-xL, Mcl-1, and survivin in a dose-dependent manner.

[1]. Kim BH, et al. MS-1020 is a novel small molecule that selectively inhibits JAK3 activity. Br J Haematol. 2010 Jan;148(1):132-43.