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C7280948 is a sulfone inhibitor of PRMT1 (IC50 values 12.75 μM and 26.7 μM, respectively, methylated substrates for oligopeptides containing human histone H4 and non-histone Npl3 1-21 amino acids). PRMT inhibitors are a potential compound and interesting tool for cell biology. C7280948 is an effective tool for studying the epigenetic effects of PRMT1. PRMT1 is also involved in activation of estrogen and androgen receptors. PRMT1 is an essential component of the oncogenic transformation induced by the mixed line leukemia (MLL) complex, and thus may represent a new research direction in hormone-dependent cancers.
| 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.
| Molecular Weight | 276.35 |
| Formula | C14H16N2O2S |
| CAS Number | 587850-67-7 |
| Purity | 100.00% |
| Solubility | DMSO 35 mg/mL |
| Storage | at -20°C |
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| GSK3368715 2HCl
GSK3368715 2HCl is a novel potent, orally active, reversible type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50 values of 3.1 nM, 48 nM, 1148 nM, 5.7 nM and 1.7 nM for PRMT1, PRMT3, PRMT4, PRMT6, PRMT8, respectively. |
| AMI-1 disodium salt
AMI-1 is a potent and selective, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50 values of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 is also a potent scavenger of NADPH-oxidase-derived superoxide. |
| HLCL-61 hydrochloride
HLCL-61 hydrochloride is a potent and selective, first-in-class protein arginine methyltransferase 5 (PRMT5) inhibitor. |
| MS049
MS049 is a potent and selective inhibitor of PRMT4,6 with IC50 values of 34 nM and 43 nM, respectively. |
| GSK3326595
GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 6.2 nM. |
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