IP6K Inhibitor – CAS 519178-28-0 – Calbiochem

Descrição detalhada : A cell-permeable 2,6-disubstituted purine compound that, although originally identified as a reversible, ATP-competitive inhibitor against the conversion of Ins(1,4,5)P3 to Ins(1,3,4,5)P4 by IP3K (IC50 = 18 M; [ATP] = 10 muM), acts in fact as a much more effective inhibitor against the IP6K1/2/3-catalyzed conversion of InsP6 (Cat. No. 407125) to 5-[PP]- InsP6 or InsP7 (IC50 = 0.47 muM against IP6K1; [ATP] = 1 mM) due to a much higher affinity of ATP toward IP3K than IP6K (Km of ATP for the respective enzymes = 0.01 vs 1000 muM). Shown to potently inhibit cellular InsP7 level (IC50 = 0.55 muM in HeLa cultures), while being less potent in increasing the cellular InsP3 accumulation (>10 M in HeLa cultures). TNP is also effective against S. cerevisiae IP6K, Kcs1, but not Vip/PPIP5Ks, enzymes that catalyze the pyrophosphorylation at the 1/3 position of InsP6 and InsP7, in either human or yeast species or two other IP3 metabolizing enzymes, PLC and IP3 5-ppase.
Sinónimos : IP6K Inhibitor - CAS 519178-28-0 - Calbiochem; N²-(m-Trifluorobenzyl), N?-(p-nitrobenzyl)purine, Inositol-1,4,5-trisphosphate 3-Kinase Inhibitor, IP3K Inhibitor, Kcs1 Inhibitor, TNP
Fórmula molecula r: C20H16F3N7O2
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X5MG