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GSK126 - ≥98%, high purity , Histone-lysine N-methyltransferase EZH2 inhibitor, CAS No.1346574-57-9, Histone-lysine N-methyltransferase EZH2 inhibitor

  • Moligand™
  • ≥98%
Item Number
G124898
Grouped product items
SKUSizeAvailabilityPrice Qty
G124898-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$70.90
G124898-10mg
10mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$105.90
G124898-50mg
50mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$284.90
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Potent and selective EZH2 methyltransferase inhibitor

View related series
enhancer of zeste 2 polycomb repressive complex 2 subunit Inhibitor

Basic Description

SynonymsGSK126|1346574-57-9|GSK-126|GSK 126|(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|GSK2816126|GSK-2816126|EZH2 inhibitor|W4OGW9QZ97|CHEMBL3287735|GSK-2816126A|1-
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsDescription:IC50 Value: 0.5nM (Ki)GSK126, a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK126 may p
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionHistone-lysine N-methyltransferase EZH2 inhibitor
NoteRefer to SDS for further information. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

GSK126 is a potent highly selective S adenosyl methionine competitive small molecule inhibitor of EZH2 methyltransferase with Ki value of 0.5 nM.

Product Properties

ALogP3.9

Associated Targets

EZH2 Tclin Histone-lysine N-methyltransferase EZH2 14 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EED Tchem Polycomb protein EED 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide
INCHI InChI=1S/C31H38N6O2/c1-6-22(5)37-18-20(3)29-25(30(38)34-17-26-19(2)13-21(4)35-31(26)39)14-24(15-27(29)37)23-7-8-28(33-16-23)36-11-9-32-10-12-36/h7-8,13-16,18,22,32H,6,9-12,17H2,1-5H3,(H,34,38)(H,35,39)/t22-/m0/s1
InChi Key FKSFKBQGSFSOSM-QFIPXVFZSA-N
Canonical SMILES CCC(C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C
Isomeric SMILES CC[C@H](C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C
PubChem CID 68210102
Molecular Weight 526.67

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Certificate of Analysis(COA)

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1 results found

Lot NumberCertificate TypeDateItem
H1518099Certificate of AnalysisMar 15, 2023 G124898

Chemical and Physical Properties

Solubility25°C: DMSO

Related Documents

 SDS

 Specification Sheet

References

1. McCabe MT, Ott HM, Ganji G, Korenchuk S, Thompson C, Van Aller GS, Liu Y, Graves AP, Della Pietra 3rd A, Diaz E et al..  (2012)  EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations..  Nature,  492  (7427): (108-12).  [PMID:23051747]

Solution Calculators

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