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]-
GSK343
CAS: 1346704-33-3
Molecular Formula: C31H39N7O2
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]- - Names and Identifiers
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]- - Physico-chemical Properties
| Molecular Formula | C31H39N7O2 |
| Molar Mass | 541.69 |
| Density | 1.26±0.1 g/cm3(Predicted) |
| Boling Point | 797.4±60.0 °C(Predicted) |
| Solubility | DMSO: soluble15mg/mL, clear |
| Appearance | powder |
| Color | , white to beige to brown |
| pKa | 11.84±0.10(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | GSK343 inhibits H3K27 (H3K27me3) trimethylation with an IC50 of 174 nM in HCC1806 lung cancer cells. GSK343 effectively inhibited cell proliferation of breast cancer cells and prostate cancer cells, and the prostate cancer cell line LNCaP was most sensitive to GSK343 with an IC50 of 2.9 μm. GSK343 significantly inhibited the growth of EOC cells cultured in a 3D artificial basement membrane extracellular matrix (ECM) that mimics the in vivo tumor microenvironment. In addition, GSK343 also induced the apoptosis of EOC cells in 3D, and significantly inhibited the invasion of EOC cells. GSK343 inhibits H3K27 (H3K27me3) trimethylation with an IC50 of 174 nM in HCC1806 lung cancer cells. GSK343 effectively inhibited cell proliferation of breast cancer cells and prostate cancer cells, and the prostate cancer cell line LNCaP was most sensitive to GSK343 with an IC50 of 2.9 μm. GSK343 significantly inhibited the growth of EOC cells cultured in a 3D artificial basement membrane extracellular matrix (ECM) that mimics the in vivo tumor microenvironment. In addition, GSK343 also induced the apoptosis of EOC cells in 3D, and significantly inhibited the invasion of EOC cells. |
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]- - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| WGK Germany | 3 |
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]- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.846 ml | 9.23 ml | 18.461 ml |
| 5 mM | 0.369 ml | 1.846 ml | 3.692 ml |
| 10 mM | 0.185 ml | 0.923 ml | 1.846 ml |
| 5 mM | 0.037 ml | 0.185 ml | 0.369 ml |
Last Update：2024-01-02 23:10:35
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]- - Reference Information
| biological activity | GSK343 is an effective, selective EZH2 inhibitor with IC50 of 4 nM, 60 times higher selectivity than EZH1 and more than 1000 times higher selectivity than other histone methyltransferase. GSK343 is an effective, selective EZH2 inhibitor. IC50 is 4 nM in cell-free test, which is 60 times more selective than EZH1 and 1000 times more selective than other histone methyltransferase. GSK343 can induce autophagy. |
| in vitro study | GSK343 inhibits H3K27 (H3K27me3) trimethylation, in HCC1806 lung cancer cells, IC50 is 174 nM. GSK343 effectively inhibits the cell proliferation of breast cancer cells and prostate cancer cells. The prostate cancer cell line LNCaP is the most sensitive to GSK343 with an IC50 of 2.9 μM. GSK343 significantly inhibited the growth of EOC cells, which were cultured in 3D artificial basement membrane extracellular matrix (ECM) that simulated the microenvironment of the tumor in vivo. In addition, GSK343 can also induce the apoptosis of EOC cells in 3D and significantly inhibit the infection of EOC cells. GSK343 inhibits H3K27 (H3K27me3) trimethylation. In HCC1806 lung cancer cells, IC50 is 174 nM. GSK343 effectively inhibits the cell proliferation of breast cancer cells and prostate cancer cells. The prostate cancer cell line LNCaP is the most sensitive to GSK343 with an IC50 of 2.9 μM. GSK343 significantly inhibited the growth of EOC cells, which were cultured in 3D artificial basement membrane extracellular matrix (ECM) that simulated the microenvironment of the tumor in vivo. In addition, GSK343 can also induce the apoptosis of EOC cells in 3D and significantly inhibit the infection of EOC cells. |
| features | a chemical probe for SGC epigenetics integration. It has potential use in a variety of solid tumors. |
| target | TargetValue EZH2 (Cell-Free Assay) 4 nM EZH1 (Cell-Free Assay) 240 nM |
| Target | Value |
| EZH2 (Cell-free assay) | 4 nM |
| EZH1 (Cell-free assay) | 240 nM |
Last Update：2024-04-09 21:11:58
![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]-](http://res.chembk.com/assets/images/structure/302188.gif)
Supplier List
Spot supply
Product Name: GSK343 Visit Supplier Webpage Request for quotationCAS: 1346704-33-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: GSK343 Visit Supplier Webpage Request for quotationCAS: 1346704-33-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History