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SGC707

Alias:

SGC707; SGC 707; SGC-707

Cat No.:V0383 Purity: ≥98%
SGC707 (SGC-707) is a novel, cell-permeable and allosteric PRMT3 inhibitor (protein arginine methyltransferase 3 inhibitor) with potential anticancer activity.
SGC707
SGC707 Chemical Structure CAS No.: 1687736-54-4
Product category: Histone Methyltransferase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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.

These protocols are for reference only. InvivoChem does not independently validate these methods.
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)
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.

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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.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • SGC707

    SGC707 binds to PRMT3 in cells and reduces PRMT3-dependent H4R3me2a. Angew Chem Int Ed Engl. 2015 Apr 20; 54(17): 5166–5170.
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