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Seclidemstat is an orally active, reversible, noncompetitive inhibitor of lysine-specific demethylase 1 (LSD1, or KDM1A) with a mean IC50 of 127 nM, it has potential antineoplastic activity. Seclidemstat suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone 3 (H3K4) to mono- and unmethylated H3K4, respectively.
In vivo, Seclidemstat reduces tumor volume at 40, 80 mg/kg by i.p. and also shows such effect at 80 mg/kg via p.o. dosing.
| 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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
| Molecular Weight | 450.94 |
| Formula | C20H23ClN4O4S |
| CAS Number | 1423715-37-0 |
| Purity | >98% |
| Solubility | DMSO ≥ 90 mg/mL |
| Storage | at -20°C |
| Related Histone demethylases Products |
|---|
| T-3775440 hydrochloride
T-3775440 hydrochloride is a potent, selecitve, irreversible LSD1 inhibitor with IC50 value of 2.1 nM. |
| GSK-J5
GSK-J5 is a cell-permeable, inactive control for histone demethylase JMJD3/UTX inhibitor GSK-J4. |
| QC6352
QC6352 is a potent KDM4C inhibitor. |
| CPI-455 HCl
CPI-455 HCl is a potent and selective inhibitor of KDM5 demethylases which reduces survival of drug-tolerant cancer cells, with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays. |
| IOX1
IOX1 is a histone demethylase inhibitor; cell permeable. IOX1 also inhibits ALKBH5. |
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