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Synonyms | EED inhibitor-1 | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C20H17FN6O |
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分子量 | 376.39 | CAS No. | 1951408-58-4 | |
Solubility (25°C)* | 体外 | 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. |
製品説明 | 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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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] |
細胞アッセイ | 細胞株 | MBCs |
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濃度 | 2 µM | |
反応時間 | 4 days, 3 days | |
実験の流れ | MBCs are differentiated using a previously described culture protocol. All cultures are performed in Iscove modified Dulbecco medium, 10% FCS and 25–35% of Resto-6 cells supernatant. 1.5 × 105/ml purified peripheral blood MBCs are activated for 4 days by 10 µg/ml of phosphorothioate CpG oligodeoxynucleotides (ODN) 2006, 50 ng/ml histidine tagged soluble CD40 ligand (CD40L) and 5 µg/ml of an anti-poly-histidine mAb in the presence of 20 U/ml IL-2, 50 ng/ml IL-10, and 10 ng/ml IL-15. The next 3 days, PBs are generated by removing ODN and CD40L and changing the cytokine cocktail. From day 7 to day 10, PBs are differentiated into early PCs by adding 50 ng/ml IL-6, 10 ng/ml IL-15, 500 U/ml IFN-α. MAK-683 (2 µM) is added at the start of each step and its effects are evaluated by analyzing cell counts and phenotype at the end of each step. |
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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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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