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Description

A cell-permeable pyrrolo-pyrazine compound that exerts anti-proliferative effects. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin-dependent kinases (Cdks, IC50 = 150 nM, 120 nM, 400 nM, and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, respectively), glycogen synthase kinase-3 (GSK-3, IC50 = 500 nM and 1.5 µ,M for GSK-3alpha, GSK-3beta, respectively), and c-Jun N-terminal kinase (JNK, IC50 = ~ 3 - 10 µ,M). It inhibits several other enzymes (CK1, CK2, MAPKK, PKA, PKG, PKCs, and c-raf) poorly (IC50 >= 100 µ,M). Shown to arrest cells in both G1 and G2 phases (IC50 = 7 µ,M and 10.5 µ,M for undifferentiated human teratocarcinoma cells NT2 and differentiated postmitotic neurons hNT, respectively). Shown to selectively stimulate CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 µ,M Forskolin (Cat. No. 344270) with high affinity (EC50 = 150 nM, 140 nM and 111 nM, respectively)., A cell-permeable, pyrrolo-pyrazine compound that exerts anti-proliferative effects. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin-dependent kinases (Cdks, IC50 = 150 nM for Cdk1/cyclin B, 120 nM for Cdk2/cyclin A, 400 nM for Cdk2/cyclin E, and 160 nM for Cdk5/p25), glycogen synthase kinase-3 (GSK-3, IC50 = 500 nM for GSK-3alpha and 1.5 µ,M for GSK-3beta), and c-Jun N-terminal kinase (JNK, IC50 ~3-10 µ,M). Also inhibits extracellular signal-regulated kinases (ERKs, IC50 = 18 µ,M for ERK1 and 22 µ,M for ERK2), PIM1 (IC50 >10 µ,M), and insulin receptor tyrosine kinase (IC50 = 60 µ,M) at higher concentrations. Does not significantly inhibit Cdk4/cyclin D1, CK1, CK2, MAPKK, PKA, PKG, PKCs, or c-raf (IC50 = >= 100 µ,M). Shown to arrest undifferentiated human teratocarcinoma cells (NT2) and differentiated post-mitotic neurons (hNT) in both G1 and G2 phases (IC50 = 7 µ,M and 10.5 µ,M, respectively). Also shown to selectively stimulate CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 µ,M of Forskolin (Cat. No. 344270) with high affinity (EC50 = 150 nM, 140 nM and 111 nM, respectively).