SGI-1027


CAS No. : 1020149-73-8

SGI-1027,1020149-73-8
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000143
Synonyms:N-[4-[(2-amino-6-methylpyrimidin-4-yl)amino]phenyl]-4-(quinolin-4-ylamino)benzamide
Molecular Formula:C₂₇H₂₃N₇O
Molecular Weight:461.52
Target:Histone Methyltransferase
IC50:6/8/7.5 uM (DNMT1/3A/3B) [1]
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Appearance:Solid powder
Purity: > 98%
Cat No:I000143
Cas No:1020149-73-8
Product-Name:SGI-1027
InChI:InChI=1S/C27H23N7O/c1-17-16-25(34-27(28)30-17)32-20-10-12-21(13-11-20)33-26(35)18-6-8-19(9-7-18)31-24-14-15-29-23-5-3-2-4-22(23)24/h2-16H,1H3,(H,29,31)(H,33,35)(H3,28,30,32,34)
InChIKey:QSYLKMKIVWJAAK-UHFFFAOYSA-N
SMILES:CC1=CC(=NC(=N1)N)NC2=CC=C(C=C2)NC(=O)C3=CC=C(C=C3)NC4=CC=NC5=CC=CC=C54

SGI-1027 is a potent and selective inhibitor of DNA methyltransferase (DNMT) with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B, respectively.
IC50 value: 6/8/7.5 uM (DNMT1/3A/3B) [1]
Target: DNMT1/3A/3B
SGI-1027, inhibits the activity of DNMT1, DNMT3A, and DNMT3B as well M. SssI with comparable IC(50) (6-13 micromol/L) by competing with S-adenosylmethionine in the methylation reaction. Treatment of different cancer cell lines with SGI-1027 resulted in selective degradation of DNMT1 with minimal or no effects on DNMT3A and DNMT3B. At a concentration of 2.5 to 5 micromol/L (similar to that of decitabine), complete degradation of DNMT1 protein was achieved within 24 h without significantly affecting its mRNA level [1].


1:Design, synthesis and biological evaluation of 4-amino-N- (4-aminophenyl)benzamide analogues of quinoline-based SGI-1027 as inhibitors of DNA methylation. Rilova E, Erdmann A, Gros C, Masson V, Aussagues Y, Poughon-Cassabois V, Rajavelu A, Jeltsch A, Menon Y, Novosad N, Gregoire JM, Vispé S, Schambel P, Ausseil F, Sautel F, Arimondo PB, Cantagrel F.ChemMedChem. 2014 Mar;9(3):590-601. doi: 10.1002/cmdc.201300420. PMID: 24678024 Free PMC Article
2:Molecular modeling studies of the novel inhibitors of DNA methyltransferases SGI-1027 and CBC12: implications for the mechanism of inhibition of DNMTs. Yoo J, Choi S, Medina-Franco JL.PLoS One. 2013 Apr 25;8(4):e62152. doi: 10.1371/journal.pone.0062152. Print 2013. PMID: 23637988 Free PMC Article
3:Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line. García-Domínguez P, Dell/'aversana C, Alvarez R, Altucci L, de Lera AR.Bioorg Med Chem Lett. 2013 Mar 15;23(6):1631-5. doi: 10.1016/j.bmcl.2013.01.085. Epub 2013 Jan 30. PMID: 23402879
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