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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 | C25H21N7O3 |
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分子量 | 467.48 | CAS No. | 371942-69-7 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 12 mg/mL (25.66 mM) | ||||||||
Water | Insoluble | ||||||||||
Ethanol | 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 | YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction of autophagy. |
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in vitro | YM201636 potently inhibits mammalian PIKfyve with an IC50 of 33 nM but not yeast orthologue Fab1 with an IC50 of >5 μM, exhibiting around 100-fold selectivity for PtdIns3P p110α with an IC50 of 3 μM. YM201636 (0.8 μM) significantly decreases the production of PtdIns(3,5)P2 by 80% in serum-starved NIH3T3 cells followed by serum stimulation with no effect on serum-stimulated protein kinase B (PKB) Ser 473 phosphorylation. YM-201636 reversibly impairs endosomal trafficking in NIH3T3 cells by blocking PIKfyve and PtdIns(3,5)P2 production, mimicking the effect produced by depleting PIKfyve with siRNA. YM-201636 (0.8 μM) also significantly reduces retroviruses budding from cells by 80%, apparently through interfering with the endosomal sorting complex required for transport (ESCRT) machinery. [1] In 3T3L1 adipocytes, YM-201636 inhibits basal and insulin-activated 2-deoxyglucose uptake with an IC50 of 54 nM, with almost complete inhibition at doses as low as 160 nM. YM-201636 (0.1 μM) has also been shown to completely block insulin-dependent activation of class IA PI 3-kinase. [2] Although not involved in NPM-ALK-dependent proliferation and migration, YM201636 (0.4 μM) strongly reduces invasive capacities of NPM-ALK-expressing cells and their capacity to degrade the extracellular matrix. [3] YM201636 treatment blocks the continuous recycling of junctional proteins claudin-1 and claudin-2 in MDCK cells, leading to the intracellular accumulation and delay of epithelial barrier formation. [4] |
キナーゼアッセイ | In vitro GST-PIKfyve assay | |
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The assay is performed in kinase buffer (25 mM HEPES pH 7.4, 120 mM NaCl, 1.5 mM MgCl2, 5 mM 2-glycerophosphate, and 1 mM DTT) containing 100 μM PI(3)P, GST-PIKfyve, 50 μM ATP/10 μCi [32P]γATP and increasing concentrations of YM201636 in a final volume of 65 μL. The reactions are incubated for 15 minutes at 30 °C, and stopped by the addition of 243 μL of 2:1 MeOH : CHCl3 (volume : volume). Lipid products labelled with 32P are analysed by thin-layer chromatography and quantified by Cerenkov counting. IC50 value is determined by using Graphpad Prism and errors are given as ±95% confidence limit. |
Data from [Data independently produced by , , FEBS Letters, 2016, 590:1576-1585.]
A loss-of-adhesion CRISPR-Cas9 screening platform to identify cell adhesion-regulatory proteins and signaling pathways [ Nat Commun, 2022, 13(1):2136] | PubMed: 35440579 |
secDrug: a pipeline to discover novel drug combinations to kill drug-resistant multiple myeloma cells using a greedy set cover algorithm and single-cell multi-omics [ Blood Cancer J, 2022, 12(3):39] | PubMed: 35264575 |
Endosome maturation links PI3Kα signaling to lysosome repopulation during basal autophagy [ EMBO J, 2022, 41(19):e110398] | PubMed: 35968799 |
Disruption of PIKFYVE causes congenital cataract in human and zebrafish [ Elife, 2022, 11e71256] | PubMed: 35023829 |
Phosphatidylinositol (3,5)-bisphosphate machinery regulates neurite thickness through neuron-specific endosomal protein NSG1/NEEP21 [ J Biol Chem, 2022, 299(1):102775] | PubMed: 36493904 |
Antiviral drug screen identifies DNA-damage response inhibitor as potent blocker of SARS-CoV-2 replication [ Cell Rep, 2021, 35(1):108940] | PubMed: 33784499 |
Epigenetic Regulation of Claudin-1 in the Development of Ovarian Cancer Recurrence and Drug Resistance [ Front Oncol, 2021, 11:620873] | PubMed: 33828978 |
Optimization of small-scale sample preparation for high-throughput OpenArray analysis [ J Biol Methods, 2021, 8(1):e143] | PubMed: 33604395 |
Genetic Screens Identify Host Factors for SARS-CoV-2 and Common Cold Coronaviruses [ Cell, 2020, S0092-8674(20)31626-3] | PubMed: 33333024 |
Dual Targeting of BRAF and mTOR Signaling in Melanoma Cells With Pyridinyl Imidazole Compounds [ Cancers (Basel), 2020, 10;12(6):E1516] | PubMed: 32531927 |
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。