SGI-1027

SKU: orb1307169

Description

SGI-1027

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1020149-73-8
• MW: 461.5
• Purity: >98%
• Formula: C₂₇H₂₃N₇O
• SMILES: Cc1cc(Nc2ccc(NC(=O)c3ccc(Nc4ccnc5ccccc45)cc3)cc2)nc(N)n1
• Target: Methyltransferase
• Solubility: Soluble in DMSO (35 mg/ml)

Bioactivity

• Target IC50:
  DNMT1:6 μM|DNMT3B:7.5 μM|DNMT3A:8 μM
• In Vivo:
  SGI-1027, at concentrations ranging from 0 to 100 μM, demonstrates moderate pro-apoptotic effects in the U937 human leukemia cell line without affecting the cell cycle. It directly inhibits DNMTs, leading to suppression of DNA methylation and selective degradation of DNMT1 across various human cancer cell lines. In the rat hepatoma H4IIE cells, SGI-1027 exhibits minimal or no toxicity.
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• Cell Research:
  Rat hepatoma H4IIE cells are used as the test system. These cells are grown in DMEM supplemented with fetal bovine serum (10%) and calf serum (10%). Cells are seeded into 96-well plates and after 48 h exposed to SGI-1027 at concentrations ranging from 0 to 300 μMol/L. The solubility is determined by Nephalometry techniques immediately after dosing and before harvesting the cells at 24 h. Following the exposure period, the cells or their supernatant (culture medium) are analyzed for changes in cell proliferation (propidium iodide), membrane leakage (α-GST), mitochondrial function [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and cellular ATP], oxidative stress (intracellular GSH and 8-isoprostane), and apoptosis. The half-maximal toxic concentration (TC50) is determined from the dose-response curves.(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DNA Methyltransferase, DNA Methyltransferase Inhibitor II, DNA methyltransferase (DNMT), DNA MTases, DNMT3A, DNMT1, DNMTs, DNMT3B, DNAMethyltransferase, Apoptosis, inhibit, Inhibitor, SGI1027, SGI-1027, SGI 1027

Compound Identifiers

PubChem CID

24858111