|
产品信息：
Form Yellow solid
Primary Target IP 3-K
Primary Target IC50 10.2 µM
Secondary target Cdk1 (IC50 > 100 µM)
Protect from Light 是的
Packaged under inert gas 是的
Cell permeable 是的
Purity ≥95% by HPLC
Chemical formula C20H16F3N7O2
CAS number 519178-28-0
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling
产品说明：
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 (Cat. Nos. 407123 & 407137) to Ins(1,3,4,5)P4 (Cat. No. 407126) by IP3K (IC50 = 18 µM; [ATP] = 10 μM), 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 μM 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 μM). Shown to potently inhibit cellular InsP7 level (IC50 = 0.55 μM in HeLa cultures), while being less potent in increasing the cellular InsP3 accumulation (>10 µM 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. |