受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C19H27N3O2 |
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分子量 | 329.44 | CAS No. | 1527503-11-2 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 65 mg/mL (197.3 mM) | ||||||||
Ethanol | 65 mg/mL (197.3 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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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. |
製品説明 | A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM and 38nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. |
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in vitro | A-366 has significantly less cytotoxic effects on the growth of tumor cell lines compared to other known G9a/GLP small molecule inhibitors despite equivalent cellular activity on methylation of H3K9me2. Treatment of various leukemia cell lines in vitro results in marked differentiation and morphological changes of these tumor cell lines[1]. |
in vivo | Treatment of a flank xenograft leukemia model with A-366 results in growth inhibition consistent with the profile of H3K9me2 reduction observed[1]. |
細胞アッセイ | 細胞株 | PC-3 prostate adenocarcinoma cells |
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濃度 | 0, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM | |
反応時間 | 72 h | |
実験の流れ | PC-3 prostate adenocarcinoma cells are incubated in triplicate with DMSO or the indicated concentrations of A-366 or UNC0638 for 72 hours. H3K9me2 levels are assessed by In-Cell Western assay. |
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動物実験 | 動物モデル | SCID-beige female mice(AML flank xenograft model) |
投薬量 | 30 mg/kg/day | |
投与方法 | by osmotic mini-pump |
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Chronic hypoxia stabilizes 3βHSD1 via autophagy suppression [ Cell Rep, 2024, 43(1):113575] | PubMed: 38181788 |
Inhibition of EHMT1/2 rescues synaptic damage and motor impairment in a PD mouse model [ Cell Mol Life Sci, 2024, 81(1):128] | PubMed: 38472451 |
Euchromatic Histone Lysine Methyltransferase 2 Inhibition Enhances Carfilzomib Sensitivity and Overcomes Drug Resistance in Multiple Myeloma Cell Lines [ Cancers (Basel), 2023, 15(8)2199] | PubMed: 37190128 |
Inhibition of the CtBP complex and FBXO11 enhances MHC class II expression and anti-cancer immune responses [ Cancer Cell, 2022, 40(10):1190-1206.e9] | PubMed: 36179686 |
BRD4770 functions as a novel ferroptosis inhibitor to protect against aortic dissection [ Pharmacol Res, 2022, 177:106122] | PubMed: 35149187 |
Inhibition of a G9a/DNMT network triggers immune-mediated bladder cancer regression. [ Nat Med, 2019, 25(7):1073-1081] | PubMed: 31270502 |
Dynamic reversal of random X-Chromosome inactivation during iPSC reprogramming. [ Genome Res, 2019, 29(10):1659-1672] | PubMed: 31515287 |
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] | PubMed: 30135193 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。