UPCDC30245 is an allosteric inhibitor of AAA ATPase p97, also called valosine containing protein (VCP). p97 is an integral component of the ubiquitin fusion degradation (UFD) pathway. It plays a role in degradation of misfolded proteins, Golgi membrane reassembly, membrane transport, myofibril assembly, autophagosome maturation, and cell division, and is overexpressed in many tumor types. UPCDC30245 has an IC50 value of 27 nM, and has been shown to bind at the junction between the D1 and D2 domains of p97. UPCDC30245 has been used in cryo-ECM to show how such inhibitor binding prevents the confomational changes necessary for p97 function.
| Molecular Weight | 463.63 |
| Formula | C28H38FN5 |
| CAS Number | 1883351-01-6 |
| Solubility (25°C) | DMSO: 30 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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