SGI-1027 | DNA methyl transferase inhibitor

CAS:
1020149-73-8
Catalog Number:
10-5488
Activity:
DNA methyl transferase inhibitor
Chemical Names:

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

Molecular Weight:
461.52
Molecular Formula:
C27H23N7O
Solubility:
Soluble in DMSO (up to 35 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$70.00
25 mg$280.00

SGI-1027 (1020149-73-8) is a 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).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 mM.1 Prolonged treatment of RKO cells resulted in reexpression of silenced tumor suppressor genes.1 Synergizes with doxorubicin at growth inhibition in neuroblastoma cell lines.2 Disrupts the MKK3-MYC complex in cells and inhibits MYC transcriptional activity in colon and breast cancer cells.3

References:

  1. Datta et al. (2009), 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., 69 4277
  2. Penter et al. (2015) A rapid screening system evaluates novel inhibitors of DNA methylation and suggests F-box proteins as potential therapeutic targets for high-risk neuroblastoma; Target Oncol., 10 523
  3. Yang et al. (2021), Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer; Bioorg. Chem., 45 116324
CAS:
1020149-73-8
Catalog Number:
10-5488
Activity:
DNA methyl transferase inhibitor
Chemical Names:

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

Molecular Weight:
461.52
Molecular Formula:
C27H23N7O
Solubility:
Soluble in DMSO (up to 35 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

20% OFF

For Postdoc
Customers!