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Formula | C20H17FN6O |
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Molecular Weight | 376.39 | CAS No. | 1951408-58-4 | |
Solubility (25°C)* | In vitro | DMSO | 12.5 mg/mL (33.21 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 | MAK683 (EED inhibitor-1, example 2) is an inhibitor of embryonic ectoderm development (EED). MAK683 exhibits IC50 of 59 nM, 89 nM and 26 nM in EED Alphascreen binding, LC-MS and ELISA assay, respectively. | ||||||
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Targets |
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In vitro | MAK-683 binds to EED and disrupts the PRC2 complex. Cell viability is not significantly affected and the levels of H3K27me3 are decreased. A significant increase in the percentage of mature PCs after MAK-683 treatment in association with a higher CD38 expression is also identified.[3] |
Cell Assay: |
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AKT and EZH2 inhibitors kill TNBCs by hijacking mechanisms of involution [ Nature, 2024, 10.1038/s41586-024-08031-6] | PubMed: 39385030 |
PPARγ and C/EBPα enable adipocyte differentiation upon inhibition of histone methyltransferase PRC2 in malignant tumors [ J Biol Chem, 2024, 300(10):107765] | PubMed: 39276936 |
Combating castration-resistant prostate cancer by co-targeting the epigenetic regulators EZH2 and HDAC [ PLoS Biol, 2023, 21(4):e3002038] | PubMed: 37104245 |
Induction of senescence-associated secretory phenotype underlies the therapeutic efficacy of PRC2 inhibition in cancer [ Cell Death Dis, 2022, 13(2):155] | PubMed: 35169119 |
ARID1A-deficient bladder cancer is dependent on PI3K signaling and sensitive to EZH2 and PI3K inhibitors [ JCI Insight, 2022, e155899] | PubMed: 35852858 |
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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.