Tubastatin A BASE | 1-(isoquinolin-6-yl)-3-(2-oxo-2-(pyrrolidin-1-yl)ethyl)urea
Specifications & Purity
Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms
SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase\u20053 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.
Storage Temp
Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
ALLOSTERIC MODULATOR
Mechanism of action
Allosteric modulator of protein arginine methyltransferase 3
Product Description
Information
SGC707 SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 ( PRMT3 ) with IC50 and K d of 31 nM and 53 nM, respectively.
Targets
PRMT3 ; PRMT3 31 nM; 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.
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.
Cell Research(from reference)
Cell lines:293, LnCap, U2O s, HFF, MCF-7, and MDA-MB-231 cells
This compound belongs to the class of organic compounds known as n-carbamoyl-alpha amino acids and derivatives. These are compounds containing an alpha amino acid (or a derivative thereof) which bears an carbamoyl group at its terminal nitrogen atom.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.