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Histone Methytransferase

SGC707 (1687736-54-4)

SGC707 is a first-in-class PRMT3 chemical probe which is a potent, selective, and cell-active allosteric inhibitor of PRMT3 with IC50 of 31 nM.

Not Intended for Therapeutic Use. For research use only.

CAS: 1687736-54-4 Category

SGC707 (1687736-54-4) Description:

SGC707 is a first-in-class PRMT3 chemical probe which is a potent, selective, and cell-active allosteric inhibitor of PRMT3 with IC50 of 31 nM. IC50 value: 31 nM Target: PRMT3 in vitro: SGC707 is the first PRMT3 chemical probe. 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). SGC707 can engage PRMT3 and effectively inhibit its catalytic activity in cells and that overexpressed PRMT3 can methylate histone H4 in cells. SGC707 stabilizes PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM in PRMT3 InCELL Hunter Assays. in vivo: SGC707 is 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. We assessed in vivo pharmacokinetic (PK) properties of SGC707. Intraperitoneal injection of SGC707 at 30 mg/kg gave good plasma exposure in CD-1 male mice over 6 h with the peak plasma level of 38000 nM. The plasma level of SGC707 at 6 h post injection was 208 nM, more than 2-fold higher than its IC50 value in the cellular assay and the half-life of SGC707 was about 1 h. This mdose was well tolerated by the test animals. These results suggest that SGC707 is suitable for animal studies in addition to cell-based studies.

SGC707 (1687736-54-4) Specifications:

Product Name SGC707
Synonyms SGC-707; SGC 707.
Chemical Name 1-isoquinolin-6-yl-3-(2-oxo-2-pyrrolidin-1-ylethyl)urea
Drug Class Inhibitor
Purity >98%
CAS Number 1687736-54-4
Molecular Formula C16H18N4O2
Molecular Weight 298.346 g/mol
Monoisotopic Mass 298.143 g/mol
MDL number N/A
InChIKey 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)
SMILES C1CCN(C1)C(=O)CNC(=O)NC2=CC3=C(C=C2)C=NC=C3
Form Powder
Color white to light brown
Solubility  DMSO: 20 mg/mL
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application PRMT3 Inhibitor

 


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RIDADR NONH for all modes of transport

References:

  • 1.Inhibition of PRMT3 activity reduces hepatic steatosis without altering atherosclerosis susceptibility in apoE knockout mice. Hoekstra M, Nahon JE, de Jong LM, Kröner MJ, de Leeuw LR, Van Eck M. Biochim Biophys Acta Mol Basis Dis. 2019 Feb 15. pii: S0925-4439(19)30064-X. doi: 10.1016/j.bbadis.2019.02.012. [Epub ahead of print]
  • 2.Inhibition of protein arginine methyltransferase 3 activity selectively impairs liver X receptor-driven transcription of hepatic lipogenic genes in vivo.  Nahon JE, Groeneveldt C, Geerling JJ, van Eck M, Hoekstra M. Br J Pharmacol. 2018 Aug;175(15):3175-3183. doi: 10.1111/bph.14361. Epub 2018 Jun 15.
  • 3.A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). 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. Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70. doi: 10.1002/anie.201412154. Epub 2015 Feb 27.

1 review for SGC707 (1687736-54-4)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The SGC707 (1687736-54-4) is high purity,also customer service is pretty nice !gotta try!!

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