A-366 is a potent and highly selective peptide-competitive inhibitor of histone methyltransferase G9a, with IC50s of 3.3 nM and 38 nM for G9a and GLP, respectively, and is more than 1,000-fold selective for G9a and GLP over 21 other methyltransferases. A-366 is also a potent inhibitor of Spindlin1-H3K4me3 interaction (IC50=182.6 nM).A-366 shows high affinity for human H3R (Ki=17 nM) and exhibits subtype selectivity between subpopulations of the histaminergic and dopaminergic receptor families. It can be used for induction and maintenance of pluripotent stem cells in mice.
Molecular Weight | 329.44 |
Formula | C19H27N3O2 |
CAS Number | 1527503-11-2 |
Form | Solid |
Solubility (25°C) | DMSO: 10 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.
[5] Xuhong Ye, et al. A gyrB-targeted PCR for rapid identification of Salmonella
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