CAS No. 1346572-63-1
| IUPAC Name | N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-[6-(4-methylpiperazin-1-yl)-3-pyridinyl]-1-propan-2-ylindole-4-carboxamide | |
|---|---|---|
| CAS Number | 1346572-63-1 | |
| Molecular Formula |
C31H38N6O2 |
|
| Molecular Weight (MW) | 526.67 | |
| SMILES | CC1=CC(=C(C(=O)N1)CNC(=O)C2=C3C(=CN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)C)C(C)C)C)C | |
| InChIKey | HRDQQHUKUIKFHT-UHFFFAOYSA-N |
GSK503 is a potent and selective inhibitor of enhancer of zeste homolog 2 (EZH2) methyltransferase. By inhibiting the catalytic activity of EZH2, the enzymatic subunit of polycomb repressive complex 2 (PRC2), this compound decreases global levels of histone H3 lysine 27 trimethylation (H3K27me3). Consequently, target gene derepression suppresses cell proliferation, impairs self-renewal, and promotes cell cycle arrest or apoptosis in EZH2-dependent cancer models. [1][2]
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Concentration
Volume
Mass
|
|---|
| Solvent | Solubility & Note |
|---|---|
| DMSO |
100 mg/mL
(189.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Ethanol | 26 mg/mL |
| Water | Insoluble |
| DMSO |
100 mg/mL
(189.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Ethanol | 4 mg/mL |
| Water | Insoluble |
| DMSO |
100 mg/mL
(189.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Ethanol | 100 mg/mL |
| Water | Insoluble |
- Preheat media/saline to 37°C.
- Mix rapidly (pipette/vortex) upon addition.
- For complex mixes, always add the aqueous phase last.
- Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).
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