GSK343

SIGMA/SML0766 - ≥98% (HPLC)

Synonym: 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

CAS Number: 1346704-33-3
Empirical Formula (Hill Notation): C₃₁H₃₉N₇O₂
Molecular Weight: 541.69
MDL Number: MFCD25563250
Linear Formula: C₃₁H₃₉N₇O₂
Product Type: Chemical

Catalog Number	PKG Qty.	Price


45-SML0766-5MG	5 mg	$148.00 1/EA	Add To Favorites
45-SML0766-25MG	25 mg	$587.00 1/EA	Add To Favorites

Properties
Descriptions
Safety Info.
Basic Data

assay	≥98% (HPLC)
color	, white to beige to brown
form	powder
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
Quality Level	100
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
solubility	DMSO: 15 mg/mL, clear
storage temp.	2-8°C

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 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 .
Features and Benefits:	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.
Packaging:	5, 25 mg in glass bottle

Symbol	GHS07
Signal word	Warning
Hazard statements	H302
Precautionary statements	P301 + P312 + P330
Hazard Codes	Xn
Risk Statements	22
RIDADR	NONH for all modes of transport
WGK Germany	WGK 3
Flash Point(F)	Not applicable
Flash Point(C)	Not applicable

Purity	≥98% (HPLC)
Storage Temp.	2-8°C
UNSPSC	12352200

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