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Merck

SML0766

GSK343

≥98% (HPLC),  histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor, powder

Synonyme(s) :

N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide, N-[(6-Methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-(propan-2-yl)-1H-indazole-4-carboxamide

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A propos de cet article

Formule empirique (notation de Hill) :
C31H39N7O2
Numéro CAS:
1346704-33-3
Poids moléculaire :
541.69
UNSPSC Code:
41106514
PubChem Substance ID:
329825594
NACRES:
NA.77
MDL number:
MFCD25563250
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100

Principaux documents

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Nom du produit

GSK343, ≥98% (HPLC)

SMILES string

CN(CC1)CCN1C2=NC=CC(C3=CC4=C(C=NN4C(C)C)C(C(NCC5=C(CCC)C=C(C)NC5=O)=O)=C3)=C2

InChI

1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40)

InChI key

ULNXAWLQFZMIHX-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

, white to beige to brown

solubility

DMSO: 15 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Catégories apparentées

Application

GSK343 has been used:
  • as an inhibitor of enhancer of zeste homolog 2 (EZH2) to assess the impact of chromatin condensation on cell migration
  • as histone methyl transferase inhibitor, to suppress the Polyandrocarpa misakiensis, mitochondrial non-coding-region (NCR) PmNCR reporter gene expression, facilitated by TC14-3
  • as a supplement in the growth medium to inhibit the generation of H3K27me3 or to inhibit RNA polymerase II
  • as EZH2 inhibitor to treat castration-resistant neuroendocrine prostate cancer (CRPC-NE)

Biochem/physiol Actions

GSK343 is a potent, specific inhibitor of the histone H3-lysine 27 (H3K27) methyltransferase EZH2.
GSK343 is a potent, specific inhibitor of the histone H3-lysine 27 (H3K27) methyltransferase EZH2. GSK343 inhibits EZH2 enzymatic activity with an IC50 of 4 nM. The compound displays 60 fold selectivity for EZH2 vs. EZH1, and 1000 fold or greater selectivity against other histone methyltransferases. The IC50 for inhibition of H3K27 methylation is < 200 nM in HCC1806 cells. For full characterization details, please visit the GSK343 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

Features and Benefits

GSK343 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Other Notes

GSK343 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK343 probe summary on the Chemical Probes Portal website.

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificats d'analyse (COA)

Lot/Batch Number
0000383557
0000383557
0000223774
0000223774
0000184411

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Consulter la Bibliothèque de documents

N A Wijetunga et al.
Oncogene, 36(14), 2030-2044 (2016-10-11)
The predisposition of patients with Hepatitis C virus (HCV) infection to hepatocellular carcinoma (HCC) involves components of viral infection, inflammation and time. The development of multifocal, genetically distinct tumours is suggestive of a field defect affecting the entire liver. The
Increased chromatin plasticity supports enhanced metastatic potential of mouse melanoma cells
Maizels Y, et al.
Experimental Cell Research, 357(2), 282-290 (2017)
Regulatory cis-and trans-elements of mitochondrial D-loop-driven reporter genes in budding tunicates
Kawamura K, et al.
Mitochondrion, 35, 59-69 (2017)
Patient derived organoids to model rare prostate cancer phenotypes
Puca L, et al.
Nature Communications, 9(1), 2404-2404 (2018)
Liduan Zheng et al.
Scientific reports, 7(1), 8967-8967 (2017-08-23)
Recent evidence shows the emerging roles of promoter-targeting endogenous microRNAs (miRNAs) in regulating gene transcription. However, miRNAs affecting the transcription of matrix metalloproteinase 14 (MMP-14) in gastric cancer remain unknown. Herein, through integrative mining of public datasets, we identified the
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