WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407283
Description: SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). SGC707 is a potent PRMT3 inhibitor (IC50 =31±2 nM, KD =53±2 nM) with outstanding selectivity (selective against 31 other methyltransferases and more than 250 non-epigenetic targets). The mechanism of action studies and crystal structure of the PRMT3-SGC707 complex confirm the allosteric inhibition mode. Importantly, SGC707 engages PRMT3 and potently inhibits its methyltransferase activity in cells. It is also bioavailable and suitable for animal studies. This well-characterized chemical probe is an excellent tool to further study the role of PRMT3 in health and disease.
MedKoo Cat#: 407283
Chemical Formula: C16H18N4O2
Exact Mass: 298.143
Molecular Weight: 298.346
Elemental Analysis: C, 64.41; H, 6.08; N, 18.78; O, 10.73
Synonym: SGC707; SGC-707; SGC 707.
IUPAC/Chemical Name: N-6-isoquinolinyl-N'-[2-oxo-2-(1-pyrrolidinyl)ethyl]-urea
SMILES Code: O=C(NCC(N1CCCC1)=O)NC2=CC3=C(C=NC=C3)C=C2
1: Kaniskan HÜ, Szewczyk MM, Yu Z, Eram MS, Yang X, Schmidt K, Luo X, Dai M, He
F, Zang I, Lin Y, Kennedy S, Li F, Dobrovetsky E, Dong A, Smil D, Min SJ, Landon
M, Lin-Jones J, Huang XP, Roth BL, Schapira M, Atadja P, Barsyte-Lovejoy D,
Arrowsmith CH, Brown PJ, Zhao K, Jin J, Vedadi M. 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. doi: 10.1002/anie.201412154.
Epub 2015 Feb 27. PubMed PMID: 25728001; PubMed Central PMCID: PMC4400258.