SGI-1027, DNA methyltransferase inhibitor (TBI5488)

Description

Product Details

Formal Name: N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide

Molecular Formula: C₂₇H₂₃N₇O

Formula Weight: 461.50

CAS Number: 1020149-73-8

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (35 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

DNA methyltransferase inhibitor

Functions

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

Application Procedures

First dissolved in DMSO (35 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.