2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 inhibits sumoylation by preventing transfer of SUMO from the UBC9-SUMO thioester to the substrate. 2-D08 is also an inhibitor of Axl with IC50 of 0.49 nM. 2-D08 decreases the ratio of p-Axl to t-Axl in a dose-dependent manner.
Molecular Weight | 270.24 |
Formula | C15H10O5 |
CAS Number | 144707-18-6 |
Solubility (25°C) | DMSO ≥ 100 mg/mL |
Storage | 2-8°C, protect from light, dry, sealed |
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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