OGG1 Inhibitor O8 is a potent inhibitor of 8-Oxoguanine DNA Glycosylase-1 (OGG1), part of the DNA base excision repair (BER) pathway that is becoming a target for cancer therapy. OGG1 Inhibitor O8 has an IC50 value of 220 nM and >100-fold selectivity for OGG1 relative to several other DNA repair glycosylases. O8 acts through the inhibition of Schiff base formation during OGG1 catalysis. It does not prevent DNA binding of OGG1 to a 7,8-dihydro-8-oxoguanine (8-oxo-Gua)-containing substrate.
| Molecular Weight | 261.13 |
| Formula | C9H6Cl2N2OS |
| CAS Number | 350997-39-6 |
| Solubility (25°C) | DMSO: 5 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.
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