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 | C33H45Cl4N3O2 |
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分子量 | 657.54 | CAS No. | 2088939-99-3 | ||||||||
Solubility (25°C)* | 体外 | Water | 100 mg/mL (152.08 mM) | ||||||||
Ethanol | 100 mg/mL (152.08 mM) | ||||||||||
DMSO | 50 mg/mL (76.04 mM) | ||||||||||
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 | LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants. |
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in vitro | LYN-1604 is a ULK1 agonist. Three amino acid residues (LYS50, LEU53, and TYR89) are key to the activation site of LYN-1604 and ULK1 by site-directed mutagenesis and biochemical assays. LYN-1604 induces cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis. LYN-1604 is bound to wild-type ULK1 with a binding affinity in the nanomole range (KD = 291.4 nM), but the ULK1Y89A mutant protein causes a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1K50A and ULK1L53A mutants[1]. |
in vivo | LYN-1604 could significantly inhibit the growth of xenograft MDA-MB-231 cells. LYN-1604 can directly activate ULK1, the initiator of autophagy, thereby inducing cell death to inhibit the growth of triple negative breast cancer (TNBC) in vitro and in vivo[1]. |
細胞アッセイ | 細胞株 | MDA-MB-231 cells |
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濃度 | 0.5, 1.0 and 2.0 μM | |
反応時間 | 24 h | |
実験の流れ | Cells are dispensed in 96-well plates at a density of 5 × 104 cells per mL. After 24 h of incubation, cells are treated with different concentrations of compounds for the indicated time periods. Cell viability is measured by the MTT assay. |
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動物実験 | 動物モデル | MDA-MB-231 xenograft model (BALB/c nude mice) |
投薬量 | 25 mg/kg, 50 mg/kg, 100 mg/kg | |
投与方法 | intragastric administration |
Piceatannol enhances Beclin-1 activity to suppress tumor progression and its combination therapy strategy with everolimus in gastric cancer [ Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9] | PubMed: 36271983 |
Synergetic contributions of viral VP1, VP3, and 3C to activation of the AKT-AMPK-MAPK-MTOR signaling pathway for Seneca Valley virus-induced autophagy [ J Virol, 2021, JVI0155021] | PubMed: 34757844 |
Corneal autophagy and ocular surface inflammation: A new perspective in dry eye. [ Exp Eye Res, 2019, 184:126-134] | PubMed: 31018117 |
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。