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With the exception of PRMT6 (IC50 = 5.2 μM), SGC2085 does not inhibit other PRMTs. Although CARM1(PRMT4) is previously shown to asymmetrically dimethylate BAF155 at R1064, no cellular activity is observed for SGC2085 when tested up to 10 μM. The absence of cellular activity for SGC2085 may due to poor permeability.
| Cell Experiment | |
|---|---|
| Cell lines | HEK293 cells |
| Preparation method | HEK293 cells are grown in 12-well plates in DMEM supplemented with 10% FBS, penicillin (100 U/mL), and streptomycin (100 μg/mL). Thirty percent confluent cells are treated with inhibitors or DMSO. After 48 h, media are removed and cells are lysed in 100 μL of total lysis buffer (20 mM Tris-HCl pH 8.0, 150 mM NaCl, 1 mM EDTA, 10 mM MgCl2, 0.5% Triton X-100, 12.5 U/mL benzonase), complete EDTA-free protease inhibitor cocktail. After 3 min incubation at room temperature, SDS is added to 1% final concentration. Lysates are run on SDS-PAGE, and immunoblotting is done as outlined below to determine the levels of unmethylated and methylated BAF155. |
| Concentrations | 10 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| 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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
| Molecular Weight | 312.41 |
| Formula | C19H24N2O2 |
| CAS Number | 1821908-48-8 |
| Purity | >98% |
| Solubility | 62 mg/mL in DMSO |
| Storage | at -20°C |
Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening.
Ferreira de Freitas R, et al. J Med Chem. 2016 Jul 28;59(14):6838-47. PMID: 27390919.
| Related Histone Methyltransferase Products |
|---|
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MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM. |
| MI-463
MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the Menin-MLL interaction, with an IC50 value of 15.3 nM. |
| MI-2
MI-2 (Menin-MLL Inhibitor 2) is a potent menin-MLL interaction inhibitor with IC50 of 446±28 nM. |
| WDR5-0103
WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM). |
| MS023
MS023 is a potent and selective, cell-active inhibitor of type I PRMTs with IC50s of 4-119 nM. |
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