S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide
1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide
CAS: 1346574-57-9
Molecular Formula: C31H38N6O2
S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide - Names and Identifiers
S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide - Physico-chemical Properties
| Molecular Formula | C31H38N6O2 |
| Molar Mass | 526.67 |
| Density | 1.25±0.1 g/cm3(Predicted) |
| Melting Point | >216°C (dec.) |
| Boling Point | 823.4±65.0 °C(Predicted) |
| Solubility | 25°C: DMSO |
| Appearance | Form Solid, color Off-White |
| pKa | 11.93±0.10(Predicted) |
| Storage Condition | -20°C Freezer |
| Physical and Chemical Properties | The bioactive GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM and is more than 1000 times more selective for EZH2 than the other 20 human methyltransferases. |
S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide - Upstream Downstream Industry
S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide - Introduction
GSK126 is a highly active, S-adenosyl-methionine competitive EZH2 methyltransferase inhibitor with Ki of 0.5 nM.
Last Update：2022-10-16 17:30:55
S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide - Uses and synthesis methods
in vitro studies
In vitro, among EZH2 wild-type and mutant DLBCL cell lines, GSK126 is the most effective in inhibiting H3K27me3, followed by H3K27me2. GSK126 can also effectively inhibit the proliferation of EZH2 mutant DLBCL cell lines and induce transcriptional activation of EZH2 target genes in sensitive cell lines. In A687V EZH2 mutant cells, GSK126 treatment resulted in decreased overall H3K27me3, activation of strong genes, activation of caspases, and decreased proliferation. In parental H2087 cells, GSK126 inhibits the expression of VEGF-A and phosphorylated Ser(473)-AK, thus causing inhibition of cell proliferation, migration and metabolism.
In vivo studies
in mice loaded with KARPAS-422 and Pfeiffer xenografts, GSK126 (150 mg/kg/d, I. p.) reduced overall H3K27me3 and increased gene expression, thus causing significant tumor regression.
Last Update：2024-04-10 22:29:15
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Product Name: GSK126 Visit Supplier Webpage Request for quotationCAS: 1346574-57-9
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View History
S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide
邻氯对苯二胺
邻氯对苯二胺
Raw Materials for S)-1-(sec-butyl)-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-3-Methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxaMide
1-(5-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)PYRIDIN-2-YL)PIPERAZINE
1H-Indole-4-carboxylic acid,6-broMo-1-(1-Methylpropyl)-,Methyl ester
2-Methyl-3-nitrobenzoic acid
5-BROMO-2-METHYL-3-NITROBENZOIC ACID
1H-Indole-4-carboxylic acid,6-broMo-1-(1-Methylpropyl)-,Methyl ester
2-Methyl-3-nitrobenzoic acid
5-BROMO-2-METHYL-3-NITROBENZOIC ACID