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YM-201636

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基本信息:

  • 发布时间: 2017-06-12
  • 产品名称: YM-201636
  • 产品英文名称: YM-201636
  • CAS号: 371942-69-7
  • 产品包装: 10mg
  • 产品价格: 2148元/罐
  • 有效期: 一年

产品图片:

YM-201636

产品描述:

YM-201636的生物活性

 

YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α.
IC50 value: 33 nM [1]
Target: PIKfyve
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].
in vivo:

 

化学信息

分子量
467.48
储存条件
参考CoA中推荐的条件进行储存。
分子式
C25H21N7O3
CAS号
371942-69-7
溶剂/溶解度
DMSO ≥33mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

 

相关文献

 

[1]. Jefferies HB, et al. A selective PIKfyve inhibitor blocks PtdIns(3,5)P(2) production and disrupts endomembrane transport and retroviral budding. EMBO Rep, 2008, 9(2), 164-170.

[2]. Ikonomov OC, et al. YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns(3,5)P2 synthesis, halts glucose entry by insulin in adipocytes. Biochem Biophys Res Commun, 2009, 382(3), 566-570.

[3]. Dupuis-Coronas S, et al. The nucleophosmin-anaplastic lymphoma kinase oncogene interacts, activates, and uses the kinase PIKfyve to increase invasiveness.J Biol Chem, 2011, 286(37), 32105-32114.

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  • 公司名称 深圳市浩博世纪生物有限公司
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