1687736-54-4

Basic information

• Product Name: SGC707
• Synonyms: SGC707;N-6-Isoquinolinyl-N'-[2-oxo-2-(1-pyrrolidinyl)ethyl]urea
• CAS NO: 1687736-54-4
• Molecular Formula: C16H18N4O2
• Molecular Weight: 298.33972
• Product Categories: API
• Mol File: 1687736-54-4.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Storage Temp.: -20°C
• Solubility: Soluble in DMSO (up to 35 mg/ml)
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
• CAS DataBase Reference: SGC707(CAS DataBase Reference)
• NIST Chemistry Reference: SGC707(1687736-54-4)
• EPA Substance Registry System: SGC707(1687736-54-4)

Safety Data

• Hazardous Substances Data: 1687736-54-4(Hazardous Substances Data)

Usage

Description

SGC707, with the chemical formula 1687736-54-4, is a potent and selective allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). It exhibits high potency with an IC50 of 31 nM and is selective against 31 other methyltransferases. SGC707 is an invaluable probe for studying the role of PRMT3 in both normal and pathophysiological conditions. It is also cell permeable and active in vivo, making it a promising compound for various applications.

Uses

Used in Pharmaceutical Research:
SGC707 is used as a research tool for investigating the role of PRMT3 in various biological processes. Its potent and selective inhibition of PRMT3 allows researchers to better understand the enzyme's function and its potential as a therapeutic target.
Used in Drug Development:
SGC707 is used as a starting point for the development of new drugs targeting PRMT3. Its potent and selective inhibition of the enzyme makes it a valuable lead compound for the creation of novel therapeutics.
Used in Cancer Research:
SGC707 is used as an anticancer agent, particularly in the study of its effects on PRMT3, which has been implicated in the development and progression of various cancers. Its potent inhibition of PRMT3 may provide insights into potential cancer treatments.
Used in Epigenetic Studies:
SGC707 is used as a probe in epigenetic research, specifically in the study of protein arginine methylation. Its selectivity for PRMT3 allows for a deeper understanding of the enzyme's role in regulating gene expression and cellular processes.
Used in Diagnostic Applications:
SGC707 may be used in the development of diagnostic tools for diseases associated with PRMT3 dysregulation. Its ability to selectively inhibit PRMT3 could potentially be leveraged to create assays for detecting abnormal PRMT3 activity in patient samples.

in vitro

the ic50 and kd value of sgc707 against prmt3was 31 ± 2 nm and 53 ± 2 nm respectively. sgc707 showed an outstanding selectivity for prmt3 against 31 other methyltransferases and a broad range of 250 non-epigenetic targets, g protein-coupled receptors (gpcrs), ion channels, and transporters. the residence time of sgc707 was 9.7 min. in both hek293 and a549 cells, sgc707 stabilized prmt3 with ec50 values of 1.3 μm and 1.6 μm, respectively. sgc707 treatment at high concentrations 50 and 100 mm for 72 h lead to some toxicity [1].

in vivo

in cd-1 male mice, intraperitoneal injection of sgc707 at 30 mg/kg for over 6 h showed good plasma exposure with the peak plasma level of 38 μm. after injection 6 h, the plasma level of sgc707 decreased to 208 nm. the half-life of sgc707 was about 1 h. the 30 mg/kg dose was well tolerated in the tested mouse model [1].

References

1) Kaniskan?et al. (2015), A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3); Angew. Chem. Int. Ed. Engl., 54?5166