CID 5380390 is a selective inhibitor of Protein Arginine Methyltransferases PRMT1 and PRMT8. PRMT1 is responsible for the majority of arginine methylation in the cell involved in transcription, chromatin modification, and signal transduction. CID 5380390 has an IC50 values of 23 μM for PRMT1, and does not inhibit PRMTs 3, 4, and 6, although it does inhibit PRMT8. The mechanism is believed to involve a specific S-adenosylmethionine (SAM)-binding cysteine present only in the Type I PRMTs PRMT1 and PRMT8 and absent in other SAM-dependent methyltransferases.
| Molecular Weight | 209.2 |
| Formula | C10H11NO4 |
| CAS Number | 37630-20-9 |
| Solubility (25°C) | DMSO 15 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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