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MilliporeSigma™ Calbiochem™ Tankyrase 1/2 Inhibitor VI, G007-LK

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50-490-70001 10 mg
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Description

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

A 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 >10μM) toward 7 other PARP enzymes (PARP1, 2, 3, 6, 7,10,11), 90 kinases, 16 phosphatases, and 75 GPCRs (IC50 >10μM). Shown to inhibit two CRC lines, COLO-320DM & SW403, colony formation in vitro (200nM) and tumor expansion in mice in vivo (20mg/kg via daily i.p.), although G007-LK toxicity is observed at higher dosages (≥30mg/kg/12 h or 60mg/kg/d via i.p.).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
TRUSTED_SUSTAINABILITY

Specifications

Color White
Description 98% by HPLC
Target Proteins Tankyrase 1/2
Molecular Formula C25H16ClN7O3S
Solubility DMSO
Content And Storage Protect from light
Form Powder
Quantity 10 mg
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