A TNKS1/2 inhibitor (IC50s = 46 and 25 nM

G007-LK – 1 mg

Brand:
Cayman
CAS:
1380672-07-0
Storage:
-20
UN-No:
De Minimis - 3077 / 9

G007-LK is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC50s = 46 and 25 nM, respectively).{40726} It is selective for TNKS1 and TNKS2 over a panel of 90 kinases, 16 phosphatases, and 73 G protein-coupled receptors (GPCRs) when used at a concentration of 10 µM. G007-LK inhibits colony formation of COLO 320 DM and SW403 colorectal cancer cell lines when used at a concentration of 200 µM, as well as human hepatocellular carcinoma (HCC) cells in a dose-dependent manner.{40727,40728} It increases expression of intestinal differentiation markers in COLO 320 DM and HCT15 cells when used at a concentration of 100 nM. G007-LK inhibits Wnt3A-induced signaling in human HEK293 and mouse 10T1/2 cells.{40727} G007-LK (20 mg/kg, i.p., twice daily) also inhibits tumor growth in COLO 320 DM and SW403 mouse xenograft models, however, it leads to intestinal toxicity when administered at a dose of 30 mg/kg twice daily, leading to moribundity and death.  

 

Available on backorder

Add to quotes
SKU: 22934 - 1 mg Category:

Description

A TNKS1/2 inhibitor (IC50s = 46 and 25 nM, respectively); selective for TNKS1 and TNKS2 over a panel of 90 kinases, 16 phosphatases, and 73 GPCRs; inhibits colony formation of COLO 320 DM and SW403 cells (200 µM); inhibits colony formation of HCC cells in a dose-dependent manner; increases differentiation marker expression in COLO 320 DM and HCT15 cells (100 nM); inhibits Wnt signaling in HEK293 and 10T1/2 cells in a dose-dependent manner; inhibits tumor growth in COLO 320 DM and SW403 mouse xenograft models (20 mg/kg, i.p., twice daily) but leads to moribundity and death at a dose of 30 mg/kg twice daily

Formal name: 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-benzonitrile

Synonyms:  Tankyrase 1/2 Inhibitor VI

Molecular weight: 530

CAS: 1380672-07-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|Wnt Signaling||Research Area|Cancer|DNA Damage and Repair|PARP||Research Area|Cell Biology|Cell Signaling|Wnt Signaling

Related products

  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 500 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 500 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 5 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 10 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 10 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 100 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page