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SGC707

Catalog No. T3084   CAS 1687736-54-4

SGC707 is a potent, selective, and cell-active allosteric inhibitor of PRMT3.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
SGC707 Chemical Structure
SGC707, CAS 1687736-54-4
Pack Size Availability Price/USD Quantity
10 mg In stock $ 59.00
25 mg In stock $ 98.00
50 mg In stock $ 195.00
100 mg In stock $ 345.00
1 mL * 10 mM (in DMSO) In stock $ 65.00
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Purity: 99.75%
Purity: 99.58%
Purity: 98.45%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SGC707 is a potent, selective, and cell-active allosteric inhibitor of PRMT3.
Targets&IC50 PRMT3:31 nM, PRMT3:53 nM(Kd)
In vitro In cells, 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. [1]
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 SGC707 is suitable for animal studies. [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 the compound in the reaction mixture in a range between 2000-0.2 nM.
Cell Research Cells are seeded in 96-well plates and treated with different concentrations of SGC707 for 72 h. Cell viability is determined using Alamar blue 0.01 mg/mL in the media. Resazurin reduction is monitored with 544 nm excitation, measuring fluorescence at 590 nm. (Only for Reference)
Molecular Weight 298.34
Formula C16H18N4O2
CAS No. 1687736-54-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 55 mg/mL (184.4 mM)

DMSO: 55 mg/mL (184.4 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Kaniskan HÜ, et al. Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compounds Library Max Bioactive Compound Library Reprogramming Compound Library Inhibitor Library Chromatin Modification Compound Library Anti-Aging Compound Library Stem Cell Differentiation Compound Library Methylation Compound Library Epigenetics Compound Library Covalent Inhibitor Library

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Keywords

SGC707 1687736-54-4 Chromatin/Epigenetic Histone Methyltransferase inhibit Inhibitor SGC 707 SGC-707 inhibitor

 

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