YM201636

製品コードS1219 バッチS121903

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₅H₂₁N₇O₃

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）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.600mg/ml (1.28mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.600mg/ml (1.28mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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. This compound (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. It 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. This chemical (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, it 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. This compound (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, it (0.4 μM) strongly reduces invasive capacities of NPM-ALK-expressing cells and their capacity to degrade the extracellular matrix. ^[3] Treatment with this chemical 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]

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.

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. This compound (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. It 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. This chemical (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, it 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. This compound (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, it (0.4 μM) strongly reduces invasive capacities of NPM-ALK-expressing cells and their capacity to degrade the extracellular matrix. ^[3] Treatment with this chemical 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]

プロトコル(参考用のみ)

キナーゼアッセイ	In vitro GST-PIKfyve assay
キナーゼアッセイ	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.

参考

https://pubmed.ncbi.nlm.nih.gov/18188180/
https://pubmed.ncbi.nlm.nih.gov/19289105/
https://pubmed.ncbi.nlm.nih.gov/21737449/

https://pubmed.ncbi.nlm.nih.gov/22396724/

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カスタマーフィードバック

: Data from [Data independently produced by , , FEBS Letters, 2016, 590:1576-1585.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Stress-induced microautophagy is coordinated with lysosome biogenesis and regulated by PIKfyve [ Mol Biol Cell, 2024, 35(5):ar70]	PubMed: 38536415
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

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。