SGI-1027 | DNA methyl transferase inhibitor

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
Weight 0.1 mg
Dimensions 0.1 × 0.1 × 0.1 cm
Size:

5 mg, 25 mg

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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

SGI-1027 | DNA methyl transferase inhibitor

$170.00$280.00

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
  • 5 mg
  • 25 mg
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