A-196 is a potent selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively, and biochemically inhibits SUV4-20 in a substrate-competitive manner. In addition, A-196 is a first-in-class chemical probe for SUV4-20, which can be used to study the role of histone methyltransferases in genome integrity.
Molecular Weight | 359.25 |
Formula | C18H16Cl2N4 |
CAS Number | 1982372-88-2 |
Form | Solid |
Solubility (25°C) | DMSO 7.18 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.
[3] Xiao-Ying Zhang, et al. Scorpion venoms in gastric cancer
[4] Yang Cao, et al. miR-196 acts as a tumor suppressor in osteosarcoma by targeting HOXA9
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