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Formula | C27H23N7O |
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Molecular Weight | 461.52 | CAS No. | 1020149-73-8 | ||||
Solubility (25°C)* | In vitro | DMSO | 68 mg/mL (147.33 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | SGI-1027 (DNA Methyltransferase Inhibitor II) is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B in cell-free assays, respectively. SGI‑1027 induces apoptosis. | ||||||
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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. [1] 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. [2] |
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In vivo | SGI-1027 (DNA Methyltransferase Inhibitor II) is a DNMT inhibitor . |
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Features | Potential for use in epigenetic cancer therapy. |
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Data from [Data independently produced by Lab Chip, 2014, 14(13), 2354-62]
Data from [Data independently produced by , , Oncol Lett, 2018, 16(5):5799-5806]
Bifunctional HDAC and DNMT inhibitor induces viral mimicry activates the innate immune response in triple-negative breast cancer [ Eur J Pharm Sci, 2024, 197:106767] | PubMed: 38636781 |
Genome-wide identification of histone lysine methyltransferases and their implications in the epigenetic regulation of eggshell formation-related genes in a trematode parasite Clonorchis sinensis [ Parasites Hosts Dis, 2024, 62(1):98-116] | PubMed: 38443774 |
DNMT3B-mediated FAM111B methylation promotes papillary thyroid tumor glycolysis, growth and metastasis [ Int J Biol Sci, 2022, 18(11):4372-4387] | PubMed: 35864964 |
Utilizing an Endogenous Progesterone Receptor Reporter Gene for Drug Screening and Mechanistic Study in Endometrial Cancer [ Cancers (Basel), 2022, 14(19)4883] | PubMed: 36230806 |
Small molecule profiling to define synergistic EGFR inhibitor combinations in head and neck squamous cell carcinoma [ Head Neck, 2022, 44(5):1192-1205] | PubMed: 35224804 |
Methionine Protects Mammary Cells against Oxidative Stress through Producing S-Adenosylmethionine to Maintain mTORC1 Signaling Activity [ Oxid Med Cell Longev, 2021, 2021:5550196] | PubMed: 34336098 |
Effect of Naoluoxintong on the NogoA/RhoA/ROCK pathway by down-regulating DNA methylation in MCAO rats [ J Ethnopharmacol, 2021, 281:114559] | PubMed: 34461189 |
Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model [ J Med Chem, 2020, 31] | PubMed: 32191458 |
Prolonged unfolded protein reaction is involved in the induction of chronic myeloid leukemia cell death upon oprozomib treatment [ Cancer Sci, 2020, 112(1):133-143] | PubMed: 33067904 |
Direct interaction of DNMT inhibitors to PrPC suppresses pathogenic process of prion. [ Acta Pharm Sin B, 2019, 9(5):952-959] | PubMed: 31649845 |
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Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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