SML0766

GSK343

≥98% (HPLC)

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₃₁H₃₉N₇O₂
• Numer CAS: 1346704-33-3
• Masa cząsteczkowa: 541.69
• Numer MDL: MFCD25563250
• Kod UNSPSC: 41106514
• Identyfikator substancji w PubChem: 329825594
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥98% (HPLC)
• Formularz: powder
• kolor: , white to beige to brown
• rozpuszczalność: DMSO: 15 mg/mL, clear
• temp. przechowywania: 2-8°C
• ciąg 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)
• Klucz InChI: ULNXAWLQFZMIHX-UHFFFAOYSA-N

Opis

Zastosowanie

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)

Działania biochem./fizjol.

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

Cechy i korzyści

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.

Inne uwagi

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.

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Informacja o środkach bezpieczeństwa

• Piktogramy: GHS07
• Hasło ostrzegawcze: Warning
• Zwroty wskazujące rodzaj zagrożenia: H302
• Zwroty wskazujące środki ostrożności: P264 - P270 - P301 + P312 - P501
• Klasyfikacja zagrożeń: Acute Tox. 4 Oral
• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable