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 |
Molecular Weight | 312.41 |
Formula | C19H24N2O2 |
CAS Number | 1821908-48-8 |
Solubility (25°C) | 56 mg/mL in DMSO |
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.
Related PRMTs Products |
---|
AMG 193
AMG 193 is an orally active inhibitor of the PRMT5/MTA complex for studies related to solid tumors. |
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 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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.