| A cell-permeable pyrazolopyrimidine compound that acts as a potent, ATP-competitive and reversible inhibitor of S6K1 (p70 ribosomal protein S6 kinase 1, IC50=9.1nM) with ~2,400 reduced activity towards Akt (IC50=22uM). Shown to completely block rpS6-Ser240/244 phosphorylation in L6 cells at 2.5uM without inducing pAkt-Thr308 and Ser473, and display substantial selectivity in a 219-kinase panel (1uM of DG2 in the presence of 10uM of ATP, IC50 50%, Clk1, Clk2, Dyrk1A, Dyrk3, Flt3, Flt3-D835Y, Flt4, GSK-3a/b, R, MAP4K4, Mink1, PKA, PRKG1, PRKG2, Ret-V804L, Ret-Y791F, RSK1, RSK3, RSK2, MSK2, MSK1 and p70S6K). Synonyms: 3-Bromo-4-(4-(2-methoxyphenyl)piperazin-1-yl)-1H-pyrazolo[3,4-d]-pyrimidine Formula: C16H17BrN6O Molecular Weight: 389.3 Solubility: DMSO (100mg/ml, clear, pale yellow solution) Purity: 97% (HPLC) Form: Supplied as an off-white solid. Storage and Stability: May be stored at 4C for short-term only. Long-term storage is recommended at -20C. Stable for 1 year after receipt. Protect from light. For maximum recovery of product, centrifuge the original vial prior to removing the cap. |
