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Formula | C31H38N6O2 |
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Molecular Weight | 526.67 | CAS No. | 1346574-57-9 | |
Solubility (25°C)* | In vitro | DMSO | 12 mg/mL (22.78 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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 | GSK126 (GSK2816126A, GSK2816126) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases. | ||
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Targets |
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In vitro | In vitro, GSK126 most potently inhibits H3K27me3, followed by H3K27me2 in both EZH2 wild-type and mutant DLBCL cell lines. GSK126 also effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines, and induces transcriptional activation of EZH2 target genes in sensitive cell lines. [1] In A687V EZH2-mutant cells, GSK126 treatment results in a global decrease in H3K27me3, robust gene activation, caspase activation, and decreased proliferation. [2] In parental H2087 cells, GSK126 inhibits the expression of VEGF-A and phosphorylated Ser(473)-AKT, and thus causes the inhibition of cell proliferation, migration and metastasis. [3] | ||
In vivo | In mice bearing KARPAS-422 and Pfeiffer xenografts, GSK126 (150 mg/kg/d, i.p.) decreases global H3K27me3, increases gene expression, and thus causes marked tumour regression. [1] |
Kinase Assay: |
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, , Br J Haematol, 2017, 178(6):936-948
Data from [Data independently produced by , , Autophagy, 2015, 11(12):2309-22.]
Data from [Data independently produced by , , Mol Cancer, 2017, 16(1):22]
Data from [Data independently produced by , , Mol Cancer Res, 2018, 16(3):417-427]
EZH2 inhibitors promote β-like cell regeneration in young and adult type 1 diabetes donors [ Signal Transduct Target Ther, 2024, 9(1):2] | PubMed: 38161208 |
A SWI/SNF-dependent transcriptional regulation mediated by POU2AF2/C11orf53 at enhancer [ Nat Commun, 2024, 15(1):2067] | PubMed: 38453939 |
Epigenetic dysregulation of eukaryotic initiation factor 3 subunit E (eIF3E) by lysine methyltransferase REIIBP confers a pro-inflammatory phenotype in t(4;14) myeloma [ Haematologica, 2024, 109(6):1893-1908] | PubMed: 38124661 |
Gamma-glutamyl transferase secreted by Helicobacter pylori promotes the development of gastric cancer by affecting the energy metabolism and histone methylation status of gastric epithelial cells [ Cell Commun Signal, 2024, 22(1):402] | PubMed: 39148040 |
Combined therapy targeting AR and EZH2 curbs castration-resistant prostate cancer enhancing anti-tumor T-cell response [ Epigenomics, 2024, 10.2217/epi-2023-0374] | PubMed: 38530086 |
EZH2 inhibition induces senescence via ERK1/2 signaling pathway in multiple myeloma [ Acta Biochim Biophys Sin (Shanghai), 2024, 56(7):1055-1064] | PubMed: 38804044 |
Select EZH2 inhibitors enhance viral mimicry effects of DNMT inhibition through a mechanism involving NFAT:AP-1 signaling [ Sci Adv, 2024, 10(13):eadk4423] | PubMed: 38536911 |
DNA hypomethylation silences anti-tumor immune genes in early prostate cancer and CTCs [ Cell, 2023, 186(13):2765-2782.e28] | PubMed: 37327786 |
DNA hypomethylation silences anti-tumor immune genes in early prostate cancer and CTCs [ Cell, 2023, 186(13):2765-2782.e28] | PubMed: 37327786 |
DNA hypomethylation silences anti-tumor immune genes in early prostate cancer and CTCs [ Cell, 2023, 186(13):2765-2782.e28] | PubMed: 37327786 |
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SHIPPING AND STORAGE
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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.