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A RAT NA,K-ATPASE B1

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号:06-170

牌:Millipore 密理博

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Replacement Information

重要规格表

Empirical Formula CAS #
C₂₀H₁₆F₃N₇O₂ 519178-28-0

价格及供货情况

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      Description
      Overview 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.
      Catalogue Number 406170
      Brand Family Calbiochem®
      Synonyms N²-(m-Trifluorobenzyl), N⁶-(p-nitrobenzyl)purine, Inositol-1,4,5-trisphosphate 3-Kinase Inhibitor, IP3K Inhibitor, Kcs1 Inhibitor, TNP
      References
      References Padmanabhan, U., et al. 2009. J. Biol. Chem. 284, 10571. Chang, Y.T., et al. 2002. ChemBioChem 3, 897.
      Product Information
      CAS number 519178-28-0
      ATP Competitive Y
      Form Yellow solid
      Hill Formula C₂₀H₁₆F₃N₇O₂
      Chemical formula C₂₀H₁₆F₃N₇O₂
      Reversible Y
      Structure formula Image Structure formula Image
      Applications
      Biological Information
      Primary Target IP 3-K
      Primary Target IC<sub>50</sub> 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
      Purity ≥95% by HPLC
      Physicochemical Information
      Cell permeable Y
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special Instructions Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

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