YM201636 |
Katalog-Nr.GC10982
One-Click Copy Product Info
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YM201636 ist ein potenter und selektiver PIKfyve-Inhibitor mit einem IC50 von 33 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 371942-69-7
Sample solution is provided at 25 µL, 10mM.
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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.
| 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. |
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| Cas No. | 371942-69-7 | SDF | |
| Chemical Name | 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 | ||
| Formula | C25H21N7O3 | M.Wt | 467.48 |
| Löslichkeit | ≥ 11.68mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1391 mL | 10.6956 mL | 21.3913 mL |
| 5 mM | 427.8 μL | 2.1391 mL | 4.2783 mL |
| 10 mM | 213.9 μL | 1.0696 mL | 2.1391 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)