SGI-1027 | DNA methyl transferase inhibitor
N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 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:
- 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
N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide
NMR (Conforms)
Safety Data Sheet:
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
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:
- 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
Related products
-
iCRT5 | Beta-catenin inhibitor
From $57.00CAS:18623-44-4Catalog Number:10-1371Activity:Beta-catenin inhibitorChemical Name:4-[5-(3,4-Dimethoxy-benzylidene)-4-oxo-2-thioxo-thiazolidin-3-yl]-butyric acidMolecular Weight:367.44Molecular Formula:C16H17NO5S2Solubility:Soluble in DMSO (up to 30 mg/ml)Physical Properties:Yellow solidPurity:98% by TLC
NMR (Conforms)Storage Temperature:-20°CStability:Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.Shipping Code:RT -
AZ3146 | Mps1 kinase inhibitor
From $60.00CAS:1124329-14-1Catalog Number:10-4778Activity:Mps1 kinase inhibitorChemical Name:9-Cyclopentyl-2-[2-methoxy-4-(1-methylpiperidine-4-yl)oxyanilino]-7-methylpurin-8-oneMolecular Weight:452.56Molecular Formula:C24H32N6O3S2Solubility:Soluble in DMSO (up to 10 mg/ml) or in Ethanol (up to at least 25 mg/ml)Physical Properties:Off-white solidPurity:98% by HPLC
NMR (Conforms)Storage Temperature:-20°Stability:Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.Shipping Code:RT -
N-Eicosanoyl serotonin | Neuroprotective
From $50.00Catalog Number:10-3631Activity:NeuroprotectiveChemical Name:Eicosanoyl-5-hydroxytryptamideAlternate Name:Eicosanoyl serotonin, EHTMolecular Weight:470.73Molecular Formula:C30H50N2O2Solubility:Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 20 mg/ml with warming)Physical Properties:Beige solidPurity:98% by TLC
NMR (Conforms)Storage Temperature:-20°Stability:Stable for 2 years from date of purchase supplied. Protect from air. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.Shipping Code:RT
Calculate the molar concentration, mass or volume in a solution.
Concentration × Volume × Molecular Weight = Mass
