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GSK126, EZH2 Methyltransferase Inhibitor.

GSK126, EZH2 Methyltransferase Inhibitor.

$129.00
GSK126 is a highly potent and selective small molecule inhibitor of histone methyltransferase EZH2.
Catalog No. Unit Price Qty
M60071-2s 2mg solid $129.00
M60071-2 10 mM in DMSO (0.380 mL) $129.00
M60071-50s 50mg solid $590.00

Details

Product Information
Molecular Weight: 526.67
Formula: C31H38N6O2
Purity: ≥98%
CAS#: 1346574-57-9
Solubility: DMSO up to 100 mM
Chemical Name: S)-1-(sec-butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

GSK126 is a highly potent and selective small molecule inhibitor of histone methyltransferase EZH2. It potently inhibits both wild-type and mutant EZH2 methyltransferase activity with similar potencies (Kiapp 0.5–3 nM), independent of substrate used, and is competitive with S-adenosylmethionine (SAM) and non-competitive with peptide substrates. GSK126 is highly selective against other methyltransferases and multiple other protein classes, even 150-fold more selective for the closest EZH1 (Kiapp89 nM) and more than 1,000-fold selective for 20 other human methyltransferases, including both SET-domain-containing and non-SET domain-containing methyltransferases. It induced a 50% loss of H3K27me3 in both EZH2 wild-type and mutant DLBCL cell lines at nM concentrations independent of EZH2 mutation status. GSK126 can decrease global H3K27me3 levels and reactivate silenced PRC2 target genes. It effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines, and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice. Pharmacological inhibition of EZH2 activity may provide a promising treatment for EZH2 mutant lymphoma.

 

How to Use:

  • In vitro:  GSK126 was used at 0.5-2 µM final concentration in vitro and in cellular assays.
  • In vivo: GSK126 was intraperitoneally (IP) dosed to mice at 50-150 mg/kg once per day, or 300 mg/kg twice per week in subcutaneous xenografts of KARPAS-422 and Pfeiffer cells.

 

Reference:

  • 1.  McCabe MT, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. (2012) Nature.492(7427):108-12.

 



Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 526.67
Formula: C31H38N6O2
Purity: ≥98%
CAS#: 1346574-57-9
Solubility: DMSO up to 100 mM
Chemical Name: S)-1-(sec-butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

GSK126 is a highly potent and selective small molecule inhibitor of histone methyltransferase EZH2. It potently inhibits both wild-type and mutant EZH2 methyltransferase activity with similar potencies (Kiapp 0.5–3 nM), independent of substrate used, and is competitive with S-adenosylmethionine (SAM) and non-competitive with peptide substrates. GSK126 is highly selective against other methyltransferases and multiple other protein classes, even 150-fold more selective for the closest EZH1 (Kiapp89 nM) and more than 1,000-fold selective for 20 other human methyltransferases, including both SET-domain-containing and non-SET domain-containing methyltransferases. It induced a 50% loss of H3K27me3 in both EZH2 wild-type and mutant DLBCL cell lines at nM concentrations independent of EZH2 mutation status. GSK126 can decrease global H3K27me3 levels and reactivate silenced PRC2 target genes. It effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines, and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice. Pharmacological inhibition of EZH2 activity may provide a promising treatment for EZH2 mutant lymphoma.

 

How to Use:

  • In vitro:  GSK126 was used at 0.5-2 µM final concentration in vitro and in cellular assays.
  • In vivo: GSK126 was intraperitoneally (IP) dosed to mice at 50-150 mg/kg once per day, or 300 mg/kg twice per week in subcutaneous xenografts of KARPAS-422 and Pfeiffer cells.

 

Reference:

  • 1.  McCabe MT, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. (2012) Nature.492(7427):108-12.

 



Products are for research use only. Not for human use.

Reviews

  1. review Review by info@xcessbio.com
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    Value

    Question:

    I tried your EZH2 hihibitors (GSK126 and EPZ6438) in xcenograft mouse models, but all the treated mice died eventually. For GSK126, we administered at 50 mg/kg I.P., and for EPZ6438, we administered at 200 mg/kg orally. I believe these 2 dose are claimed to be safe according to both your data sheets and the papers that published these 2 compounds. So I am wondering what may cause the toxicities and how pure these compounds are.

     

    Our answer and solution:

    Xcessbio is the first company to launch GSK126 and EPZ6438 globally. We have supplied more than 20 different in vivo studies and people are continuing to buy from us and all said the drugs worked very well. The drug's purity is very high, all > 98%. Because GSK126 is a chiral compound, we believe we are still the only vendor to provide it with >98% ee for chirality.  Our COA documents, NMR, HPLC data can be requested by emailing info@xcessbio.com with lot number.

    In this special case, the customer may have encountered some other difficulties as demonstrated by our QC documents.

    We have in vivo study experts to be your consultant.  There are many reasons for mice death in an experiment.  For example, it is not the drug's toxicity but the tumors that actually causes the death, the dosing formulation and dosing volume used for IP and PO might be critical, the IP injection and PO dosing handling is important too (do you have standard SOP for these operation)? To consult with our in vivo study expert or for any trouble shooting, detailed formulation, dosing volume and dosing procedure should be provided through email info@xcessbio.com, an CDA shall be sighed before the procedure if the info is confidential.  We would like to help case by case. 

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