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网站主页 化工产品目录 生物化工 抑制剂 PI3K/Akt/mTOR抑制剂(PI3K/Akt/mTOR) PI3K 抑制剂 6-氨基-N-[3-[4-(4-吗啉基)吡啶并[3',2':4,5]呋喃并[3,2-D]嘧啶-2-基]苯基]-3-吡啶甲酰胺 YM-201636
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YM-201636

YM-201636
广东 更新日期:2017-06-12

深圳市浩博世纪生物有限公司

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产品详情:

中文名称:
YM-201636
英文名称:
YM-201636
CAS号:
371942-69-7

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.

公司简介

深圳市浩博世纪生物有限公司位于深圳市龙岗区,是一家专业从事科研用生化试剂及相关产品销售的公司; 产品涉及生化试剂、化学试剂、抗体、对照标准品、ELISA试剂盒、细胞培养试剂、常用耗材及小仪器等;致力于为生物企业、科研院所、大专院校等提供全方位的科研实验服务。 公司与国内外知名企业,科研院校和多家代理商建立了良好的合作关系,是国内产品系列多,品种全,质量优的生物产品和生化试剂供应商。能够满足各生物企业、科研院所、医疗机构的各种需求,能长期提供一站式试剂供应服务。

成立日期 (9年)
注册资本 10万元人民币
员工人数 1-10人
年营业额 ¥ 100万以内
经营模式 贸易,试剂,服务
主营行业 化学试剂,通用试剂,格氏试剂,绿色化学产品,基础有机试剂

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