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YM-201636

YM201636 是是一种特异性 PIKfyve 抑制剂，IC50值为 33 nM，对 p110α的IC50为 3.3 μM。它还可抑制逆转录病毒复制。

CAS号

371942-69-7

分子式

C25H21N7O3

主要靶点

Autophagy|PI3K|Influenza Virus

仅限科研使用

Cat No : CM05993

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Synonyms

验证数据展示

  • CAS No.: 371942-69-7

    YM-201636
    CAS#: 371942-69-7

产品信息

YM201636 (IC50=33 nM), a specific PIKfyve inhibitor, is less effective to p110α and insensitive to Fabl, which is yeast orthologue.

CAS号 371942-69-7
分子式 C25H21N7O3
主要靶点 Autophagy|PI3K|Influenza Virus
主要通路 自噬|PI3K/Akt/mTOR信号通路|微生物学
分子量 467.48
纯度 97.28%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

PIKfyve:33 nM

体内活性

在血清饥饿处理的NIH3T3细胞中, YM201636（0.8 μM）明显降低PtdIns(3,5)P2产量,降低达 80%。在3T3L1脂肪细胞中,YM-201636（IC50=54 nM）抑制2-脱氧葡萄糖吸收, 按160 nM剂量处理时,则能够完全抑制2-脱氧葡萄糖吸收。在MDCK细胞中,YM201636细胞间隙连接蛋白Claudin-1和Claudin-2的连续再循环,导致细胞内累积,也延迟上皮屏障的形成。

溶解度

DMSO:33 mg/mL (70.6 mM),H2O:<1 mg/mL,Ethanol:<1 mg/mL

细胞实验

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].

参考文献

1.Jefferies HB, et al. EMBO Rep, 2008, 9(2), 164-170.
2.Ikonomov OC, et al. Biochem Biophys Res Commun, 2009, 382(3), 566-570.
3.Dupuis-Coronas S, et al. J Biol Chem, 2011, 286(37), 32105-32114.
4.Dukes JD, et al. PLoS One, 2012, 7(3), e28659.

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