IP6K INHIBITOR - CAS 519178-28-0 - CALBIOCHEM

General description

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 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 (K_m 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 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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
IP 3-K

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.47 µM against IP6K1; [ATP] = 1 mM; 18 µM against the conversion of Ins(1,4,5)P3 to Ins(1,3,4,5)P4 by IP3K; [ATP] = 10 µM

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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