Inositol-1,4,5-trisphosphate 3-Kinase Inhibitor
N2-(m-Trifluorobenzyl), N6-(p-nitrobenzyl)purine Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable 2,6-disubstituted purine compound that acts as a selective, ATP-competitive inhibitor of IP 3-K (IC50 = 10.2 µM), the kinase that catalyzes the conversion of IP3 (Cat. Nos. 407123 and 407137) to IP4 (Cat. No. 407126). Induces elevated cellular IP3 level and Ca2+-release in a dose-dependent manner (5 to 20 µM in HL60 cells). Exhibits negligible inhibitory effect on Cdk1 (IC50 >100 µM) and two other IP3 metabolizing enzymes, PLC and IP3 5-ppase, even at concentrations as high as 200 µM. Useful alternative to the non-cell-permeable IP3 or IP3 analogs for studies involving intact cells. Purity: ≥95% by HPLC. CAS 519178-28-0. Ref.: Chang, Y.T., et al. 2002. ChemBioChem 3, 897. |
