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Merck

SML0766

Sigma-Aldrich

GSK343

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

Synonym(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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About This Item

Empirical Formula (Hill Notation):
C31H39N7O2
CAS Number:
1346704-33-3
Molecular Weight:
541.69
MDL number:
MFCD25563250
UNSPSC Code:
41106514
PubChem Substance ID:
329825594
NACRES:
NA.77

Key Documents

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Product Name

GSK343, ≥98% (HPLC)

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

, white to beige to brown

solubility

DMSO: 15 mg/mL, clear

storage temp.

2-8°C

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

Related Categories

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

Signal Word

Warning

Hazard Statements

H302

Precautionary Statements

P264 - P270 - P301 + P312 - P501

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
017M4634V
105M4732V
045M4717V
104M4701V
073M4616V

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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)
Loredana Puca et al.
Nature communications, 9(1), 2404-2404 (2018-06-21)
A major hurdle in the study of rare tumors is a lack of existing preclinical models. Neuroendocrine prostate cancer is an uncommon and aggressive histologic variant of prostate cancer that may arise de novo or as a mechanism of treatment
Patient derived organoids to model rare prostate cancer phenotypes
Puca L, et al.
Nature Communications, 9(1), 2404-2404 (2018)
Regulatory cis-and trans-elements of mitochondrial D-loop-driven reporter genes in budding tunicates
Kawamura K, et al.
Mitochondrion, 35, 59-69 (2017)
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We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

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