I-138 is an orally active, potent reversible inhibitor of USP1-UAF1, structurally related to ML323, showing synergistic binding to ubiquitin and mutually exclusive binding to ML323. I-138 induces mono-ubiquitination of FANCD2 and PCNA in MDA-MB-436 cells, increases PCNA and FANCD2 mono-ubiquitination in HAP-1 USP1 WT cells, and abrogates USP1 auto-cleavage in cells.
| Molecular Weight | 492.5 |
| Formula | C26H23F3N6O |
| CAS Number | 2098211-50-6 |
| Form | Solid |
| 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.
[2] E WOJTEK. Arztl Forsch. [The reaction of eosinophils after experimental carotid sinus block]
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