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504907 Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem

Tankyrase 1/2 Inhibitor VI, G007-LK, CAS 1380672-07-0, is a cell-permeable, potent and highly selective inhibitor of tankyrase (IC50 = 33 & 26 nM for TNKS1 and TNKS2, respectively).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4-(5-((E)-2-(4-(2-Chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)ethenyl)-1,3,4-oxadiazol-2-yl)benzonitrile, TNKS1/2 Inhibitor VI, G007LK, Wnt Pathway Inhibitor XXI

Primary Target: Tankyrase 1/2
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504907
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Overview

Key Spec Table

CAS #Empirical Formula
1380672-07-0C₂₅H₁₆ClN₇O₃S

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      Description
      OverviewA cell-permeable, triazolyl-vinyl-oxadiazole compound that targets adenosine site of the NAD+ pocket in the TNKS PARP domain and acts as a potent and highly selective tankyrase inhibitor (IC50 = 33 and 26 nM, respectively, against TNKS1/PARP5a/ARTD5 and TNKS2/PARP5b/ARTD6 in auto-PARsylation assays), effectively inhibiting murine Wnt3a-induced reporter activity in human HEK293 and murine 10T1/2 cultures (ICmax ~300 and 600 nM, respectively). Shown to display little or no inhibitory potency (IC50 >10 µM) toward 7 other PARP enzymes (PARP1, 2, 3, 6, 7,10,11), 90 kinases, 16 phosphatases, and 75 GPCRs (IC50 >10 µM). Shown to inhibit two CRC lines, COLO-320DM & SW403, colony formation in vitro (200 nM) and tumor expansion in mice in vivo (20 mg/kg via daily i.p.), although G007-LK toxicity is observed at higher dosages (≥30 mg/kg/12 h or 60 mg/kg/d via i.p.).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number504907
      Brand Family Calbiochem®
      Synonyms4-(5-((E)-2-(4-(2-Chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)ethenyl)-1,3,4-oxadiazol-2-yl)benzonitrile, TNKS1/2 Inhibitor VI, G007LK, Wnt Pathway Inhibitor XXI
      References
      ReferencesLau, T., et al. 2013. Cancer Res. 73, 3132.
      Voronkov, A., et al. 2013. J. Med. Chem. 56, 3012.
      Product Information
      CAS number1380672-07-0
      FormWhite powder
      Hill FormulaC₂₅H₁₆ClN₇O₃S
      Chemical formulaC₂₅H₁₆ClN₇O₃S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationTankyrase 1/2 Inhibitor VI, G007-LK, CAS 1380672-07-0, is a cell-permeable, potent and highly selective inhibitor of tankyrase (IC50 = 33 & 26 nM for TNKS1 and TNKS2, respectively).
      Biological Information
      Primary TargetTankyrase 1/2
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      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 InstructionsFollowing 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
      Global Trade Item Number
      Catalogue Number GTIN
      5.04907.0001 04055977263657