YM-201636
作者：齊岳
發(fā)布時(shí)間：2023-09-11
09:27:46
點(diǎn)擊數(shù)：
產(chǎn)品名稱：YM-201636
產(chǎn)品描述：
| 產(chǎn)品描述 | YM201636 (IC50=33 nM), a specific PIKfyve inhibitor, is less effective to p110α and insensitive to Fabl, which is yeast orthologue. |
| 靶點(diǎn)活性 | PIKfyve:33 nM |
| 體內(nèi)活性 | 在血清饑餓處理的NIH3T3細(xì)胞中, YM201636（0.8 μM）明顯降低PtdIns(3,5)P2產(chǎn)量,降低達(dá) 80%。在3T3L1脂肪細(xì)胞中,YM-201636（IC50=54 nM）抑制2-脫氧葡萄糖吸收, 按160 nM劑量處理時(shí),則能夠完全抑制2-脫氧葡萄糖吸收。在MDCK細(xì)胞中,YM201636細(xì)胞間隙連接蛋白Claudin-1和Claudin-2的連續(xù)再循環(huán),導(dǎo)致細(xì)胞內(nèi)累積,也延遲上皮屏障的形成。 |
| 激酶實(shí)驗(yàn) | Following 3T3L1 adipocyte serum-starvation and insulin stimulation, cell lysates containing protease inhibitors are clarified and then subjected to immunoprecipitation with anti-PIKfyve antibodies. Washed beads are mixed with 100 μM PtdIns and preincubated for 15 min with YM-201636 (100 nM) or vehicle in the assay buffer (50 mM Tris-HCl, pH 7.5, 1 mM EGTA and 10 mM MgCl2). The kinase assay (50 μL final volume) is carried out for 15 min at 37 °C with 15 μM ATP and [γ-32P]ATP (30 μCi). Lipids are extracted, spotted on TLC glass plates (250 μm), resolved by a chloroform/methanol/water/ammonia solvent system and detected by autoradiography[2]. |
| 細(xì)胞實(shí)驗(yàn) | YM-201636 is dissolved in DMSO and diluted with DMEM and added to cells at a final concentration of 800 nM. Cells are treated with YM-201636 or a DMSO control for 2 h. For TER measurements cells are plated at confluency on Transwell permeable polyester filters (0.4 μM pore size) with surface area of 0.33 cm2. Media is changed ever 2-3 days and cells are grown for 7 days prior to TER measurements[4]. |
| 分子量 | 467.48 |
| 分子式 | C25H21N7O3 |
| CAS No. | 371942-69-7 |
存儲
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: <1 mg/mL
DMSO: 33 mg/mL (70.6 mM)
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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