SGC707 (SGC-707) is a novel, cell-permeable and allosteric PRMT3 inhibitor (protein arginine methyltransferase 3 inhibitor) with potential anticancer activity. It inhibits PRMT3 with an IC50 and a Kd of 31 nM and 53 nM, respectively. PRMT3 is involved in cancer development via interaction with the DAL-1 tumor suppressor protein. SGC707 is a chemical probe acting by inhibiting the activity of PRMT3 via targeting the dimerization interface of PRMT3.

Physicochemical Properties

Molecular Formula	C16H18N4O2
Molecular Weight	298.34
Exact Mass	298.142
CAS #	1687736-54-4
Related CAS #	1687736-54-4
PubChem CID	90642938
Appearance	Light yellow to yellow solid powder
Density	1.3±0.1 g/cm3
Boiling Point	538.5±46.0 °C at 760 mmHg
Flash Point	279.5±29.0 °C
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.677
LogP	0.94
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	3
Heavy Atom Count	22
Complexity	409
Defined Atom Stereocenter Count	0
InChi Key	DMIDPTCQPIJYFE-UHFFFAOYSA-N
InChi Code	InChI=1S/C16H18N4O2/c21-15(20-7-1-2-8-20)11-18-16(22)19-14-4-3-13-10-17-6-5-12(13)9-14/h3-6,9-10H,1-2,7-8,11H2,(H2,18,19,22)
Chemical Name	N-6-isoquinolinyl-N-[2-oxo-2-(1-pyrrolidinyl)ethyl]-urea
Synonyms	SGC707; SGC 707; SGC-707
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	In HEK293 and A549 cells, SGC707 (0-10 μM; 6 hours) binds PRMT3 [1].
ln Vivo	In LDL receptor knockout mice given a Western diet, SGC707 (ip; 10 mg/kg; three times per week; three weeks) therapy decreases plasma triglyceride levels and produces pruritus [2].
Cell Assay	Cell Viability Assay[1] Cell Types: HEK293 and A549 cells Tested Concentrations: 0-10 μM Incubation Duration: 6 hrs (hours) Experimental Results: Stabilized PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM, respectively.
Animal Protocol	Animal/Disease Models: Western-type diet-fed LDL (lipoprotein) receptor knockout mice[2] Doses: 10 mg/kg Route of Administration: intraperitoneal (ip)injection; 10 mg/kg; 3 times per week; 3 weeks Experimental Results: demonstrated 50% lower liver triglyceride stores as well as 32% lower plasma triglyceride levels.
References	[1]. A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70. [2]. PRMT3 inhibitor SGC707 reduces triglyceride levels and induces pruritus in Western-type diet-fed LDL receptor knockout mice. Sci Rep. 2022 Jan 10;12(1):483.

Solubility Data

Solubility (In Vitro)

DMSO: 59 mg/mL (197.7 mM) Water:<1 mg/mL Ethanol:59 mg/mL (197.7 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 3 mg/mL (10.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (10.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 3 mg/mL (10.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.3519 mL	16.7594 mL	33.5188 mL
	5 mM	0.6704 mL	3.3519 mL	6.7038 mL
	10 mM	0.3352 mL	1.6759 mL	3.3519 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.