N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide

ChemicalBook > CAS DataBase List > N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide

N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide

Product Name: N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
CAS No.: 1346572-63-1
Chemical Name: N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
Synonyms: GSK03;GSK503;CS-1698;GSK-503;GSK 503;GSK-503,EZH2 inhibitor;GSK-503;GSK503;GSK 503;GSK-503,Inhibitor,inhibit,GSK503,GSK 503,Histone Methyltransferase;N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide;N-[(4,6-Dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide;1H-Indole-4-carboxamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-
CBNumber: CB72738845
Molecular Formula: C31H38N6O2
Formula Weight: 526.67
MOL File: 1346572-63-1.mol

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N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide Property

Boiling point:: 798.6±60.0 °C(Predicted)
Density: 1.24±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: ≥21.65 mg/mL in DMSO; insoluble in H2O; ≥26.85 mg/mL in EtOH with gentle warming
form: solid
pka: 11.93±0.10(Predicted)
color: White to gray

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML2718
Product name: GSK503
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $97.4
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML2718
Product name: GSK503
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $316
Updated: 2024/03/01

Cayman Chemical

Product number: 18531
Product name: GSK503
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 18531
Product name: GSK503
Purity: ≥98%
Packaging: 5mg
Price: $139
Updated: 2024/03/01

Cayman Chemical

Product number: 18531
Product name: GSK503
Purity: ≥98%
Packaging: 10mg
Price: $243
Updated: 2024/03/01

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N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide Chemical Properties,Usage,Production

Uses

GSK503 is an EZH2 inhibitor for treating cancer.

Biological Activity

gsk503 is a potent inhibitor of ezh2.enhancer of zeste homolog 2 (ezh2) is a histone-lysine n-methyltransferase enzyme that catalyses trimethylation of lysine 27 in histone 3 (h3k27me3), and then induces chromatin compaction and consequently inhibits target genes transcription.gsk503 is a potent ezh2 inhibitor with anticancer activity. in human melanoma cells, gsk503 significantly reduced h3k27me3 levels, induced g1 cell cycle arrest and slowed down cell growth [1].in mice, gsk503 induced reversible weight loss by ~10%. in mice with skin melanomas, gsk503 reduced h3k27me3 levels in tumour and stromal cells, and significantly reduced the emergence of new skin melanomas. also, gsk503 significantly inhibited the proliferation of tumour cells. in c57bl/6 mice xenografted murine b16-f10 melanoma cells, gsk503 significantly reduced h3k27me3 levels and inhibited tumor growth. also, gsk503 inhibited lymph node and lung metastases of melanoma and reduced lung nodule counts. gsk503 increased the expression of deoxycytidine kinase (dck), adenosylmethionine decarboxylase 1 (amd1) and wd repeat domain 19 (wdr19), which were ezh2 target genes [1].

References

[1]. zingg d, debbache j, schaefer sm, et al. the epigenetic modifier ezh2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors. nat commun, 2015, 6: 6051.

N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide Preparation Products And Raw materials

Raw materials

Preparation Products

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N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide Suppliers

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1346572-63-1, N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamideRelated Search:

RET Kinase inhibitor 1 GSK484 GSK583 GSK369796 GSK461364 GSK547 GSK-467 GSK481 GSK-3326595 4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide

N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide

GSK503

GSK03

GSK-503,EZH2 inhibitor

N-[(4,6-Dimethyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-3-methyl-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide

GSK-503;GSK503;GSK 503

GSK-503;GSK 503

CS-1698

1H-Indole-4-carboxamide, N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-

GSK-503,Inhibitor,inhibit,GSK503,GSK 503,Histone Methyltransferase

1346572-63-1

Inhibitors

API