SGC707 is a first-in-class PRMT3 chemical probe which is a potent, selective, and cell-active allosteric inhibitor of PRMT3 with IC50 of 31 nM. SGC707 binds to PRMT3 and reduces PRMT3-dependent H4R3me2a. SGC707 also stabilizes PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM, respectively. SGC707 (30 mg/kg, i.p.) gives good plasma exposure over 6 h with the peak plasma level of 38000 nM in CD-1 male mice, which suggests that SGC707 is suitable for animal studies.
|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||DMSO 50 mg/mL
Ethanol 50 mg/mL
A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
Kaniskan HÜ, et al. Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70. PMID: 25728001.
|Related Histone Methyltransferase Products|
MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM.
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 (Menin-MLL Inhibitor 2) is a potent menin-MLL interaction inhibitor with IC50 of 446±28 nM.
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 is a potent and selective, cell-active inhibitor of type I PRMTs with IC50s of 4-119 nM.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.