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Cat. No. M3008
SGI-1027 Structure

DNA Methyltransferase Inhibitor II

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 90  USD90 In stock
5mg USD 55  USD55 In stock
10mg USD 100  USD100 In stock
50mg USD 330  USD330 In stock
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Quality Control
Biological Activity

SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B

Customer Product Validations & Biological Datas
Source Front Neurosci (2016). Figure 6. SGI-1027
Method RT-PCR
Cell Lines Magnetic-Activated Cell Sorting
Concentrations 10 μM
Incubation Time 24 h
Results Our results show that SGI-1027 allows the sustained expression of Oct4 after retinal injury, only in the GLAST-positive fraction of retinas
Cell Experiment
Cell lines Rat hepatoma H4IIE cells
Preparation method Using the rat hepatoma H4IIE cells as the test system. These cells are grown in DMEM which is supplemented with fetal bovine serum (10%) and calf serum (10%). Cells are seeded into 96-well plates , 48 h later exposed them to SGI-1027 ,which concentrations are 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. Determine the half-maximal toxic concentration (TC50) from the dose-response curves.
Concentrations ~300 μM
Incubation time 48 hours
Animal Experiment
Animal models
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 461.52
Formula C27H23N7O
CAS Number 1020149-73-8
Purity >99%
Solubility DMSO 25 mg/mL
Storage at -20°C
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Keywords: SGI-1027, DNA Methyltransferase Inhibitor II supplier, DNA Methyltransferase, inhibitors

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