MS023 potently inhibits PRMT1 (IC50 = 30 ± 9 nM), PRMT3 (IC50 = 119 ± 14 nM), PRMT4 (IC50 = 83 ± 10 nM), PRMT6 (IC50 = 4 ± 0.5 nM), and PRMT8 (IC50 = 5 ± 0.1 nM). MS023 displays high potency for type I PRMTs including PRMT1, -3, -4, -6, and -8 but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. MS023 potently decreases cellular levels of histone arginine asymmetric dimethylation. It also reduces global levels of arginine asymmetric dimethylation and concurrently increased levels of arginine monomethylation and symmetric dimethylation in cells.
| Cell Experiment | |
|---|---|
| Cell lines | MCF7, U2Os, HFF, HCT116, HEK293 , A549, MDA-MB-231 and T98G |
| Preparation method | Different cell lines are seeded on 96-well plates at density 3000/well and treated with MS023 at 0, 0.1, 1, 10, 50 and 100 μM concentrations for 96 h. MCF7, U2Os, HFF, HCT116, HEK293 are grown in DMEM and A549, MDA-MB-231 and T98G in RPMI supplemented with 10% FBS, penicillin (100 U/mL) and streptomycin (100 mg/mL). The inhibitor is replaced after 48 h. The confluency is measured using IncuCyte™ ZOOM live cell imaging device and analysed with IncuCyte™ ZOOM (2015A) software based on phase contrast images. |
| Concentrations | ~100 μM |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 287.40 |
| Formula | C17H25N3O |
| CAS Number | 1831110-54-3 |
| 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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| PRMT5-IN-2
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| SGC2085 hydrochloride
SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins. |
| PF-06939999
PF-06939999 (PRMT5-IN-3) is a PRMT5 inhibitor that is synthetically lethal to tumor cells in combination with DNA damaging agents. |
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