SML0766

GSK343

≥98% (HPLC)

• 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
• Formule empirique (notation de Hill): C₃₁H₃₉N₇O₂
• Numéro CAS: 1346704-33-3
• Poids moléculaire : 541.69
• Numéro MDL: MFCD25563250
• Code UNSPSC : 41106514
• ID de substance PubChem : 329825594
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: powder
• Couleur: , white to beige to brown
• Solubilité: DMSO: 15 mg/mL, clear
• Température de stockage: 2-8°C
• Chaîne SMILES: 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)
• Clé InChI: ULNXAWLQFZMIHX-UHFFFAOYSA-N

Description

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)

Actions biochimiques/physiologiques

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

Caractéristiques et avantages

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.

Autres remarques

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.

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H302
• Conseils de prudence: P264 - P270 - P301 + P312 - P501
• Classification des risques: Acute Tox. 4 Oral
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable