GSK 343
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- CAS-Nr.
- 1346704-33-3
- Englisch Name:
- GSK 343
- Synonyma:
- GSK343;CS-728;GSK-343;GSK 343;GSK343, >=98%;GSK-343/GSK343;GSK 343 USP/EP/BP;GSK343, 10 mM in DMSO;GSK343;GSK 343;GSK-343;GSK343, histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor
- CBNumber:
- CB52666625
- Summenformel:
- C31H39N7O2
- Molgewicht:
- 541.69
- MOL-Datei:
- 1346704-33-3.mol
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GSK 343 Eigenschaften
- Siedepunkt:
- 797.4±60.0 °C(Predicted)
- Dichte
- 1.26±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- L?slichkeit
- DMSO: soluble15mg/mL, clear
- Aggregatzustand
- powder
- pka
- 11.84±0.10(Predicted)
- Farbe
- , white to beige to brown
- InChIKey
- ULNXAWLQFZMIHX-UHFFFAOYSA-N
- 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
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Kennzeichnung gef?hrlicher |
Xn |
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| R-S?tze: |
22 |
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| WGK Germany |
3 |
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| Speicherklasse |
11 - Combustible Solids |
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| Hazard Classifications |
Acute Tox. 4 Oral |
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| Bildanzeige (GHS) |
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| Alarmwort |
Warnung
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| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H302 |
Gesundheitssch?dlich bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 4 |
Warnung |
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P264, P270, P301+P312, P330, P501 |
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| Sicherheit |
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GSK 343 Chemische Eigenschaften,Einsatz,Produktion Methoden
Verwenden
GSK343 has been used:
- as an inhibitor ofenhancer of zeste homolog 2 (EZH2) to assess the impact of chromatin condensation oncell migration
- as histone methyl transferase inhibitor, to suppress the Polyandrocarpa misakiensis, mitochondrial non-coding-region (NCR) PmNCRreporter gene expression, facilitatedby 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
GSK 343 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
GSK 343 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 180)Lieferanten
1346704-33-3()Verwandte Suche:
- 1H-Indazole-4-carboxamide, N-[(1,2-dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-
- 1-(1-Methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide GSK343
- GSK 343
- GSK-343
- GSK-343/GSK343
- 1-(1-Methylethyl)-N-[(6-Methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)Methyl]-6-[2-(4-Methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxaMide
- N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-py
- 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-
- GSK343, >=98%
- 1-Isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazi
- GSK 343 USP/EP/BP
- CS-728
- 1-isopropyl-n-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)m Ethyl]-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1h-indazole-4-c Arboxamide
- GSK343;GSK 343;GSK-343
- N-((2-hydroxy-6-methyl-4-propylpyridin-3-yl)methyl)-1-isopropyl-6-(2-(4-methylpiperazin-1-yl)pyridin-4-yl)-1H-indazole-4-carboxamide
- N-[(6-METHYL-2-OXO-4-PROPYL-1H-PYRIDIN-3-YL)METHYL]-6-[2-(4-METHYLPIPERAZIN-1-YL)PYRIDIN-4-YL]-1-PROPAN-2-YLINDAZOLE-4-CARBOXAMIDE
- 1-Isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazin-1-yl)pyridin-4-yl)-1H-indazole-4-carboxamide
- 1-(1-Methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-6-[2-(4-methyl-1-piper
- GSK343, histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor
- GSK343, 10 mM in DMSO
- GSK343
- 1346704-33-3
- C31H39N7O2
- API
- Inhibitors
