SGI-1027
Description Features In vitro- Product Name
- SGI-1027
- CAS No.
- 1020149-73-8
- Chemical Name
- SGI-1027
- Synonyms
- CS-1144;SGI-1027;SGI1027; SGI 1027;SGI-1027 USP/EP/BP;DNA Methyltransferase Inhibitor II;N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide;N-[4-[(2-amino-6-methylpyrimidin-4-yl)amino]phenyl]-4-(quinolin-4-ylamino)benzamide;Benzamide, N-[4-[(2-amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)-;N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide SGI-1027;SGI-1027 N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide
- CBNumber
- CB42663344
- Molecular Formula
- C27H23N7O
- Formula Weight
- 461.52
- MOL File
- 1020149-73-8.mol
SGI-1027 Property
- Melting point:
- >280℃
- Density
- 1.387±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- Soluble in DMSO (up to 35 mg/ml)
- pka
- 13.31±0.70(Predicted)
- form
- powder
- color
- white to light brown
- Stability:
- Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
N-Bromosuccinimide Price
- Product number
- SML1358
- Product name
- SGI-1027
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $142
- Updated
- 2023/06/20
- Product number
- SML1358
- Product name
- SGI-1027
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $564
- Updated
- 2023/06/20
- Product number
- 11165
- Product name
- SGI-1027
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 11165
- Product name
- SGI-1027
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $108
- Updated
- 2024/03/01
- Product number
- 11165
- Product name
- SGI-1027
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $178
- Updated
- 2024/03/01
SGI-1027 Chemical Properties,Usage,Production
Description
SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B in cell-free assays, respectively.
Features
Potential for use in epigenetic cancer therapy.
In vitro
SGI-1027 inhibits DNA methylation by directly inhibiting DNMTs, and results in selective degradation of DNMT1 in a wide variety of human cancer cell lines. SGI-1027 exhibits minimal or no cytotoxic effect in rat hepatoma H4IIE cells. SGI-1027 (0-100 μM) exhibits a moderate pro-apoptotic effect on U937 human leukemia cell line with no relevant changes on the cell cycle.
Description
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
Uses
SGI-1027 is a quinoline derivative and a potent inhibitor of DNA methyltransferase (DNMT). SGI-1027 can be used as a potential therapeutic agent for the treatment of cancer and other diseases and also as a research tool to investigate the role of DNMTs in epigenetic events.
Biochem/physiol Actions
SGI-1027 is a DNA methyltransferase (DNMT) inhibitor with IC50 values of 6-13 μM for DNMT3B, DNMT3A and DNMT1. SGI-1027 directly inhibits DNMT activity by competing with the cofactor, S-adenosylmethionine (SAM) in the methylation reaction. SGI-1027 treatment of cancer cell lines induced degradation of DNMT1, but not DNMT3A or DNMT3B, and in RKO cells caused re-expression of the silenced tumor supressor genes p16, MLH1 and TIMP3.
target
DNMT1
storage
Store at -20°C
References
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 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 Yang et al. (2021), Discovery of the first chemical tools to regulate MKK3-mediated MYC activation in cancer; Bioorg. Chem., 45 116324
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