Description Features In vitro
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SGI-1027

Description Features In vitro
SGI-1027 Structure
SGI-1027
  • CAS No.1020149-73-8
  • Chemical Name:SGI-1027
  • CBNumber:CB42663344
  • Molecular Formula:C27H23N7O
  • Formula Weight:461.52
  • MOL File:1020149-73-8.mol
SGI-1027 Property
  • Melting point >280℃
  • Density 1.387±0.06 g/cm3(Predicted)
  • storage temp. 2-8°C
  • solubility Soluble in DMSO (up to 35 mg/ml)
  • pka 13.31±0.70(Predicted)
  • form powder
  • color white to light brown
  • Stability Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
  • UNSPSC Code 12352200
  • NACRES NA.77
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements
SGI-1027 Price More Price(2)
  • Brand: Sigma-Aldrich(India)
  • Product number: SML1358
  • Product name : SGI-1027
  • Purity: ≥98% (HPLC)
  • Packaging: 5MG
  • Price: ₹13908.3
  • Updated: 2022/06/14
  • Buy: Buy
  • Brand: Sigma-Aldrich(India)
  • Product number: SML1358
  • Product name : SGI-1027
  • Purity: ≥98% (HPLC)
  • Packaging: 25MG
  • Price: ₹55932.9
  • Updated: 2022/06/14
  • Buy: Buy

SGI-1027 Chemical Properties,Usage,Production

  • Description SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B in cell-free assays, respectively.
  • Features Potential for use in epigenetic cancer therapy.
  • In vitro SGI-1027 inhibits DNA methylation by directly inhibiting DNMTs, and results in selective degradation of DNMT1 in a wide variety of human cancer cell lines. SGI-1027 exhibits minimal or no cytotoxic effect in rat hepatoma H4IIE cells.  SGI-1027 (0-100 μM) exhibits a moderate pro-apoptotic effect on U937 human leukemia cell line with no relevant changes on the cell cycle.
  • Description SGI-1027 (1020149-73-8) is a potent and selective inhibitor of DNA methyl transferase inhibiting DNMT1, DNMT3A and DNMT3B with comparable potency (IC50=12.5, 8.0 and 7.5 mM respectively).1? Treatment of various cancer cell lines with SGI-1027 results in selective degradation of DNMT1 (MG-132 sensitive) with minimal effect on DNMT3A and 3B at 2.5-5 mM.1 Prolonged treatment of RKO cells resulted in reexpression of silenced tumor suppressor genes.1 Synergizes with doxorubicin at growth inhibition in neuroblastoma cell lines.2 Disrupts the MKK3-MYC complex in cells and inhibits MYC transcriptional activity in colon and breast cancer cells.3
  • Uses SGI-1027 is a quinoline derivative and a potent inhibitor of DNA methyltransferase (DNMT). SGI-1027 can be used as a potential therapeutic agent for the treatment of cancer and other diseases and also as a research tool to investigate the role of DNMTs in epigenetic events.
  • Biochem/physiol Actions SGI-1027 is a DNA methyltransferase (DNMT) inhibitor with IC50 values of 6-13 μM for DNMT3B, DNMT3A and DNMT1. SGI-1027 directly inhibits DNMT activity by competing with the cofactor, S-adenosylmethionine (SAM) in the methylation reaction. SGI-1027 treatment of cancer cell lines induced degradation of DNMT1, but not DNMT3A or DNMT3B, and in RKO cells caused re-expression of the silenced tumor supressor genes p16, MLH1 and TIMP3.
  • target DNMT1
  • storage Store at -20°C
  • References Datta et al. (2009), A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation; Cancer Res., 69 4277 Penter et al. (2015) A rapid screening system evaluates novel inhibitors of DNA methylation and suggests F-box proteins as potential therapeutic targets for high-risk neuroblastoma; Target Oncol., 10 523 Yang et al. (2021), Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer; Bioorg. Chem., 45 116324
SGI-1027 Preparation Products And Raw materials
Raw materials
Preparation Products
SGI-1027 Suppliers
Global(101)Suppliers
  • Supplier：
    TargetMol Chemicals Inc.
  • Tel：+1-781-999-5354<br/>+1-00000000000
  • Email：marketing@targetmol.com
  • Country：United States
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  • Supplier：
    Career Henan Chemica Co
  • Tel：+86-0371-86658258<br/>+8613203830695
  • Email：laboratory@coreychem.com
  • Country：China
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  • Supplier：
    InvivoChem
  • Tel：+1-708-310-1919<br/>+1-13798911105
  • Email：sales@invivochem.cn
  • Country：United States
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  • Supplier：
    Coresyn Pharmatech Co., Ltd.
  • Tel：+86-571-86626709<br/>+86-18157142896
  • Email：cbc@coresyn.com
  • Country：China
  • ProdList：9984
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  • Supplier：
    LEAPCHEM CO., LTD.
  • Tel：+86-852-30606658
  • Email：market18@leapchem.com
  • Country：China
  • ProdList：43340
  • Advantage：58
SGI-1027 Spectrum
1020149-73-8, SGI-1027Related Search:
  • Inhibitors
  • 抑制剂
  • 合成有机化合物配体
  • 细胞生物学试剂
  • 小分子抑制剂，天然产物
  • 小分子抑制剂
  • C27H23N7O
  • DNA甲基转移酶抑制剂(DNMT抑制剂)
  • 化合物SGI-1027,10 MM DMSO 溶液
  • SGI 1027,DNA甲基转移酶抑制剂
  • SGI1027游离
  • 化合物SGI-1027
  • N-[4-[(2-氨基-6-甲基-4-嘧啶基)氨基]苯基]-4-(4-喹啉基氨基)苯甲酰胺
  • 1020149-73-8
  • SGI-1027, 10 mM in DMSO
  • SGI-1027 USP/EP/BP
  • SGI1027; SGI 1027
  • CS-1144
  • SGI-1027 N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide
  • N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide SGI-1027
  • Benzamide, N-[4-[(2-amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)-
  • DNA Methyltransferase Inhibitor II
  • N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide
  • SGI-1027
  • N-[4-[(2-amino-6-methylpyrimidin-4-yl)amino]phenyl]-4-(quinolin-4-ylamino)benzamide

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