GSK-LSD1 dihydrochloride induces gene expression changes in cancer cell lines with average EC50 of < 5 nM and inhibits cancer cell line growth with average EC50 of < 5 nM.
 |
Source | Oncotarget (2017). Figure 4. GSK-LSD1 |
| Method | LDH activity assay | |
| Cell Lines | HSC-3 cells | |
| Concentrations | 1 and 10 μM | |
| Incubation Time | 24 and 48 hours | |
| Results | Thus, GSK-LSD1 inhibits EGF-induced signaling and proliferation without cytotoxicity in oral cancer cells. This represents a potential mechanism for the inhibitory effects of GSK-LSD1. |
| Molecular Weight | 289.24 |
| Formula | C14H22Cl2N2 |
| CAS Number | 2102933-95-7 |
| Solubility (25°C) | 50 mM in water 100 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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