SGI-1027

Aliases: N-[4-[2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-quinolinylamino)benzamide
Catalog No: 14150 Format: 25 mg $640 Add to Cart
Catalog No: 14151 Format: 5 mg $165 Add to Cart
Application: Histone Acetylation (HAT & HDAC)

Chemical Properties


MW = 464.5
C27H23N7O
CAS 1020149-73-8
>98% (HPLC); NMR (Conforms)

Description

Potent and selective inhibitor of DNA methyl transferase inhibiting DNMT1, DNMT3A and DNMT3B with comparable potency (IC50=12.5, 8.0 and 7.5 M respectively) (ref 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 M (ref 1). Prolonged treatment of RKO cells resulted in reexpression of silenced tumor suppressor genes (ref 1). Synergizes with doxorubicin at growth inhibition in neuroblastoma cell lines (ref 2). Disrupts the MKK3-MYC complex in cells and inhibits MYC transcriptional activity in colon and breast cancer cells (ref 3).

Contents

Off-White powder. May be dissolved in DMSO (35 mg/ml).

Storage Conditions

Store desiccated as supplied at room temperature for up to 1 year. Store solutions at -20°C for up to 2 months.

References

1. J Datta et al. Cancer Res. 2009 69:4277
2. L Penter et al. Target Oncol. 2015 10:523
3. X Yang et al. Bioorg. Med. Chem. 2021 45:116324

 
Chemical Structure of SGI-1027.

Chemical Structure of SGI-1027