GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity. Upon administration, GSK2879552 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the dimethylated form of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor-suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. LSD1, overexpressed in certain tumor cells, plays a key role in tumor cell growth and survival.
MedKoo Cat#: 206158
Name: GSK2879552
CAS#: 1401966-69-5 (free)
Chemical Formula: C23H28N2O2
Exact Mass: 364.2151
Molecular Weight: 364.49
Elemental Analysis: C, 75.79; H, 7.74; N, 7.69; O, 8.78
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 1.0 | 2.74 | |
| DMSO | 35.0 | 96.02 | |
| PBS (pH 7.2) | 5.0 | 13.72 |
The following data is based on the product molecular weight 364.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
