YM201636
(Synonyms: 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) 目录号 : GC10982
Inhibitor of PIKfyve
Cas No.:371942-69-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1, 2]: | |
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Cell lines |
Mouse 3T3L1 adipocytes, NIH3T3 cells |
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Preparation method |
The solubility of this compound in DMSO is >11.7mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0-4 μM for 30 min or 800 nM for 2h |
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Applications |
In mouse 3T3L1 adipocytes, YM201636 significantly inhibited both basal and insulin-activated 2DG uptake in a dose-dependent way. YM201636 (160 nM) nearly completely inhibited the net insulin effect with a 50% inhibition at 54 ± 4 nM. YM201636 at 800 nM produced a 45% inhibition of cell surface HA-GLUT4-eGFP accumulation and a 55% inhibition of Akt-Ser473 phosphorylation. In NIH3T3 cells, YM201636 at 800 nM decreased PtdIns(3,5)P2 production by 80%. YM201636 induced the vesiculation phenotype by affecting PIKfyve and PtdIns(3,5)P2 production. |
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References: [1] Jefferies H B J, Cooke F T, Jat P, et al. A selective PIKfyve inhibitor blocks PtdIns (3, 5) P2 production and disrupts endomembrane transport and retroviral budding. EMBO reports, 2008, 9(2): 164-170. [2]. Ikonomov O C, Sbrissa D, Shisheva A. YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns (3, 5) P2synthesis, halts glucose entry by insulin in adipocytes. Biochemical and biophysical research communications, 2009, 382(3): 566-570. | |
YM201636 is a potent, selective and cell-permeable inhibitor of mammalian class III phosphatidylinositol phosphate kinase PIKfyve with IC50 value of 33nM [1].
The pyridofuropyrimidine compound, YM201636, is a small-molecule inhibitor of PIKfyve. In the in vitro assay, it inhibits PIKfyve with IC50 value of 33nM and shows no inhibition of yeast orthologue of PIKfyve. It inhibits PtdIns3P p110α and type Iα PtdInsP kinase with IC50 values of 3μM and > 2μM, respectively. The type IIγ PtdInsP kinase is found to be insensitive to YM201636. In serum-starved NIH3T3 cells, YM201636 inhibits PtdIns (3, 5) P2 production by 80% at concentration of 800nM. Acute treatment of YM201636 to MEFs, MDCK, MCF10A, COS7 and NIH3T3 cells causes the formation of large vesicular structures. Besides that, YM201636 is also found to reduce the Akt phosphorylation and GLUT4 cell surface translocation through inhibiting the insulin-dependent class I PI 3k activation [1, 2].
References:
[1] Jefferies H B J, Cooke F T, Jat P, et al. A selective PIKfyve inhibitor blocks PtdIns (3, 5) P2 production and disrupts endomembrane transport and retroviral budding. EMBO reports, 2008, 9(2): 164-170.
[2] Ikonomov O C, Sbrissa D, Shisheva A. YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns (3, 5) P2synthesis, halts glucose entry by insulin in adipocytes. Biochemical and biophysical research communications, 2009, 382(3): 566-570.
| Cas No. | 371942-69-7 | SDF | |
| 别名 | 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 | ||
| 化学名 | 6-amino-N-[3-(4-morpholin-4-ylpyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenyl]pyridine-3-carboxamide | ||
| Canonical SMILES | C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)NC(=O)C6=CN=C(C=C6)N | ||
| 分子式 | C25H21N7O3 | 分子量 | 467.48 |
| 溶解度 | ≥ 11.68mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1391 mL | 10.6956 mL | 21.3913 mL |
| 5 mM | 0.4278 mL | 2.1391 mL | 4.2783 mL |
| 10 mM | 0.2139 mL | 1.0696 mL | 2.1391 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。