Home Epigenetics Histone Methyltransferase inhibitor - PRMT inhibitor SGC707

research use only

SGC707 Histone Methyltransferase inhibitor

Cat.No.S7832

SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.
SGC707 Histone Methyltransferase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 298.34

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 298.34 Formula

C16H18N4O2

 Storage (From the date of receipt)
CAS No. 1687736-54-4 Download SDF Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CCN(C1)C(=O)CNC(=O)NC2=CC3=C(C=C2)C=NC=C3

Solubility

In vitro
Batch:

DMSO : 59 mg/mL (197.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 59 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
PRMT3 [1]
31 nM
PRMT3 [1]
53 nM(Kd)
In vitro
In cells, SGC707 binds to PRMT3 and reduces PRMT3-dependent H4R3me2a. This compound also stabilizes PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM, respectively. [1]
Kinase Assay
PRMT3 biochemical assay
A radioactivity-based assay is optimized and used to determine the inhibition of PRMT3 in vitro. In a scintillation proximity assay (SPA), tritiated S-adenosylmethionine (3H-SAM) served as a methyl donor to methylate biotinylated histone peptide substrate. After completion of the reaction, the reaction mixture is transferred to the wells of a streptavidin / scintillant-coated microplate. The Biotinylated peptides binding to streptavidin coated resin, brings the incorporated 3H-methyl and the scintillant to close proximity. The amount of methylated peptide is quantified by tracing the radioactivity (counts per minute) as measured by the TopCount NXT™ Microplate Scintillation and Luminescence Counter. Due to the very acidic nature of the 3H-SAM solution, non-tritiated (cold) SAM is used to supplement the reactions. The C-terminally biotinylated peptide composed of the first 24 amino acids residues of histone H4 (H4 1-24) is used as substrate. The typical assay mixture contained 0.01% Tween-20, 5 mM DTT, 20 nM PRMT3, 0.3 µM B-H4 1-24 and 28 µM (5 µM 3H-SAM plus 23 µM cold SAM) SAM in 20 mM Tris-HCl (pH 7.5) and a final volume of 20 µL. The IC50 values are determined at Km concentrations of both substrates by titration of this compound in the reaction mixture in a range between 2000-0.2 nM.
In vivo
In CD-1 male mice, SGC707 (30 mg/kg, i.p.) gives good plasma exposure over 6 h with the peak plasma level of 38000 nM, which suggests that this compound is suitable for animal studies. [1]
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map