KDM2A/7A-IN-1 is a first-in-class, selective, cell-permeable inhibitor of the histone lysine demethylase KDM2A/7A, with an IC50 value of 0.16 μM for KDM2A, 75-fold more selective than other JmjC lysine demethylases, and with no effect on methyltransferases or histone acetyltransferases. KDM2A was 75 times more selective than other JmjC lysine demethylases and had no effect on methyltransferases and histone acetyltransferases.
| Molecular Weight | 506.68 |
| Formula | C33H38N4O |
| CAS Number | 2169272-46-0 |
| Form | Solid |
| Solubility (25°C) | DMSO >100 mg/mL |
| 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.
| Related Histone demethylase Products |
|---|
| INCB059872
INCB059872 is a potent, orally active, selective and irreversible inhibitor of lysine-specific demethylase 1 (LSD1) in myeloid leukemia. |
| NCD38 TFA
NCD38 TFA is a LSD1-selective inhibitor. |
| LSD1-IN-26
LSD1-IN-26 is a potent LSD1 inhibitor, with an IC50 of 25.3 nM. |
| JMJD6-IN-1
JMJD6-IN-1 is a JMJD6 inhibitor, with an inhibition rate of 82% at 10 μM. |
| LSD1-IN-25
LSD1-IN-25 is a potent, selective and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM). |
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