IP6K Inhibitor-CAS 519178-28-0-Calbiochem

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一般描述

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)P₃to Ins(1,3,4,5)P₄by IP3K (IC₅₀= 18 M; [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]- InsP₆or InsP₇(IC₅₀= 0.47 μM against IP6K1; [ATP] = 1 mM) due to a much higher affinity of ATP toward IP3K than IP6K (K_mof ATP for the respective enzymes = 0.01 vs 1000 μM). Shown to potently inhibit cellular InsP₇level (IC₅₀= 0.55 μM in HeLa cultures), while being less potent in increasing the cellular InsP₃accumulation (>10 M in HeLa cultures). TNP is also effective againstS. cerevisiaeIP6K, Kcs1, but not Vip/PPIP5Ks, enzymes that catalyze the pyrophosphorylation at the 1/3 position of InsP₆and InsP₇, in either human or yeast species or two other IP3 metabolizing enzymes, PLC and IP3 5-ppase.

包装

5 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Product competes with ATP.
Reversible: yes
Primary Target
IP 3-K
Target IC₅₀: 0.47 ?M against IP6K1; [ATP] = 1 mM; 18 ?M against the conversion of Ins(1,4,5)P3 to Ins(1,3,4,5)P4 by IP3K; [ATP] = 10 ?M

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Padmanabhan, U., et al. 2009.J. Biol. Chem.284,10571.Chang, Y.T., et al. 2002.ChemBioChem3,897.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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