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 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.|
|Incubation time||48 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||62 mg/mL in DMSO|
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.
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MS023 is a potent and selective, cell-active inhibitor of type I PRMTs with IC50s of 4-119 nM.
BIX-01294 is a potent chemical inhibitor of G9a methyltransferase that catalyzes the mono-and di-methylation of the lysine 9 residue of histone H3, with IC50 of 1.9 μM.
EPZ011989 is a potent, orally-available EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646.
SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells.
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