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SGI 1027 dihydrochloride
- S 1027 dihydrochloride
- Parent CAS: 1020149-73-8
- Soluble in DMSO
- MF: C27H25Cl2N7O
- MW: 534.44
Description
SGI 1027 dihydrochloride is a DNA methyltransferase inhibitor with reported IC50 values of 35 μM for DNMT1 and 10 μM for the DNMT3A2/3L complex. Prolonged treatment induces DNA demethylation and re-expression of silenced tumor suppressor genes including P16, MLH1 and TIMP3.
Aberrant DNA methylation contributes to epigenetic silencing of tumor suppressor genes in cancer. SGI 1027 is useful for studying DNMT inhibition, epigenetic reprogramming and reactivation of methylation-silenced gene expression.
Key Features
- DNMT1 and DNMT3A2/3L inhibitor
- IC50: 35 μM at DNMT1 and 10 μM at DNMT3A2/3L
- Promotes demethylation of silenced tumor suppressor genes
- Reported additional affinity for GLP/G9a-like protein
Applications
- DNA methylation research
- Epigenetic cancer studies
- Tumor suppressor gene reactivation assays
- DNMT inhibitor profiling
More Information
| Parent CAS No. | 1020149-73-8 |
|---|---|
| Chemical Name | N-(4-(2-amino-6-methylpyrimidin-4-ylamino)phenyl)-4-(quinolin-4-ylamino)benzamide dihydrochloride |
| SMILES | C(NC1=CC=C(NC2C=C(C)N=C(N)N=2)C=C1)(=O)C1=CC=C(NC2C3C(N=CC=2)=CC=CC=3)C=C1.Cl.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C27H23N7O.2ClH/c1-17-16-25(34-27(28)30-17)32-20-10-12-21(13-11-20)33-26(35)18-6-8-19(9-7-18)31-24-14-15-29-23-5-3-2-4-22(23)24;;/h2-16H,1H3,(H,29,31)(H,33,35)(H3,28,30,32,34);2*1H |
| InChiKey | YHBVRBOEKSJVML-UHFFFAOYSA-N |
| CID | 91826513 |
| Short Description | DNMT inhibitor |
References
- S. Valente et al. Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells. J. Med. Chem. 2014, 57, 701-713.
- E. Rilova 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, 9, 590-601.
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