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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.

同义词: TNKS1/2 Inhibitor VI, G007LK, Wnt Pathway Inhibitor XXI, 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

Primary Target: Tankyrase 1/2
504907
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概述

重要规格表

CAS #Empirical Formula
1380672-07-0C₂₅H₁₆ClN₇O₃S

Products

产品目录编号包装 数量 / 包装
5.04907.0001 玻璃瓶 10 mg
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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®
SynonymsTNKS1/2 Inhibitor VI, G007LK, Wnt Pathway Inhibitor XXI, 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
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
产品目录编号 GTIN
5.04907.0001 04055977263657