Free shipping on all orders over $ 500

SGI-1027

Cat. No. M3008
SGI-1027 Structure
Synonym:

DNA Methyltransferase Inhibitor II

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 65  USD65 In stock
5mg USD 55  USD55 In stock
10mg USD 100  USD100 In stock
50mg USD 330  USD330 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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
Protocol (for reference only)
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
Formulation
Dosages
Administration
Chemical Information
Molecular Weight 461.52
Formula C27H23N7O
CAS Number 1020149-73-8
Solubility (25°C) DMSO 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] J J Li, et al. Effects of SGI-1027 on Formation and Elimination of PrP^(Sc) in Prion-Infected Cells

[2] Ning Sun, et al. DNMTs inhibitor SGI-1027 induces apoptosis in Huh7 human hepatocellular carcinoma cells

[3] Elodie Rilova, et al. Design, synthesis and biological evaluation of 4-amino-N- (4-aminophenyl)benzamide analogues of quinoline-based SGI-1027 as inhibitors of DNA methylation

[4] Jakyung Yoo, et al. Molecular modeling studies of the novel inhibitors of DNA methyltransferases SGI-1027 and CBC12: implications for the mechanism of inhibition of DNMTs

[5] Patricia Garca-Domnguez, et al. Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line

Related DNA Methyltransferase Products
(S)-GSK-3685032

(S)-GSK-3685032 is the inactive isomer of GSK-3685032.GSK-3685032 is a non-time-dependent, non-covalent, first-in-class, reversible selective inhibitor of DNMT1 with an IC50 value of 0.036 μM.GSK-3685032 induces DNA GSK-3685032 induces loss of DNA methylation, transcriptional activation and cancer cell growth inhibition.

(R)-GSK-3685032

(R)-GSK-3685032 is the R-isomer of GSK-3685032.GSK-3685032 is a non-time-dependent, non-covalent, first-in-class, reversible selective inhibitor of DNMT1 with an IC50 value of 0.036 μM.GSK-3685032 induces DNA GSK-3685032 induces loss of DNA methylation, transcriptional activation and cancer cell growth inhibition.

DNMT-IN-1

DNMT-IN-1 is a potent DNMT inhibitor with an EC50 value of 3.2 µM.

DNMT2-IN-1

DNMT2-IN-1 is a potent and selective DNMT2 (DNA methyltransferase 2) inhibitor with an IC50 value of 1.2 μM, and has the potential for mental and metabolic disorders or cancer research.

Guadecitabine

Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS).

  Catalog
Abmole Inhibitor Catalog




Keywords: SGI-1027, DNA Methyltransferase Inhibitor II supplier, DNA Methyltransferase, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.