SGI-1027

SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly (dI-dC) as substrate.

Product Specifications

CAS Number

[1020149-73-8]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; DNA Methyltransferase

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/SGI-1027.html

Concentration

10mM

Purity

99.92

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(NC1=CC=C(NC2=NC(N)=NC(C)=C2)C=C1)C3=CC=C(NC4=CC=NC5=CC=CC=C45)C=C3

Molecular Formula

C27H23N7O

Molecular Weight

461.52

Precautions

H302, H315, H319, H335

References & Citations

[1]Datta J, et al. 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. 2009 May 15;69 (10) :4277-85.|[2]Rilova E, 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. ChemMedChem. 2014 Mar;9 (3) :590-601.