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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 |
| Related PRMTs Products |
|---|
| AMG-193
AMG-193 is an orally active inhibitor of the PRMT5/MTA complex for studies related to solid tumors. AMG-193 (PRMT5-IN-27) inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM. |
| AZD3470
AZD3470 is a novel PRMT5 inhibitor targeting the MTA and PRMT5 complex for studies related to hematologic tumors. |
| TNG-462
TNG-462 is an orally active PRMT5 inhibitor for investigation of MTAP-deficient and/or MTA-accumulating cancers. |
| TNG908
TNG908 (Ralometostat) is a PRMT5 inhibitor that crosses the blood-brain barrier and can be used in studies related to advanced solid tumors. |
| PRMT5-IN-20
PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity. |
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