YM-201636
Based on 16 publication(s) in Google Scholar
YM-201636 is a potent and selective PIKfyve inhibitor with an IC50 of 33 nM. YM-201636 also inhibits p110α with an IC50 of 3.3 μM. YM-201636 inhibits retroviral replication.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.07%
- CAS. Nr.: 371942-69-7
- Formel: C25H21N7O3
- Molecular Weight:467.48
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) YM-201636
More- Nat Commun. 2023 Jan 14;14(1):226. [Abstract]
- Nat Commun. 2020 Mar 27;11(1):1620. [Abstract]
- eGastroenterology. 2026 Mar 31;4(1):e100348. [Abstract]
- Ecotoxicol Environ Saf. 2021 Nov 19:228:112993. [Abstract]
- J Thromb Haemost. 2020 Jul;18(7):1756-1772. [Abstract]
- Molecules. 2020 Apr 23;25(8):1980. [Abstract]
- PLoS Pathog. 2025 Aug 4;21(8):e1013342. [Abstract]
- PLoS Pathog. 2025 Jan 2;21(1):e1012800. [Abstract]
- J Biol Chem. 2024 Jun 03.
- J Virol. 2020 Nov 23;94(24):e01570-20. [Abstract]
- J Med Virol. 2023 Feb;95(2):e28527. [Abstract]
- BMC Immunol. 2020 Jan 17;21(1):3. [Abstract]
- Biochem Biophys Res Commun. 2025 Feb 2:747:151123. [Abstract]
- Asian Pac J Allergy Immunol. 2023 Jun 11. [Abstract]
- bioRxiv. 2023 Aug 12.
- Res Sq. 2023 Aug 30:rs.3.rs-3154465. [Abstract]
Customer Validation & Images
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RT-PCR
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IF
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RT-PCR
Biologische Aktivität
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PIKfyve 33 nM (IC50) |
p110α 3.3 μM (IC50) |
Autophagy |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | EC50 |
400 nM
Compound: YM201636
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Induction of swollen vesicle phenotype in mouse NIH3T3 cells incubated for 120 mins by time-lapse analysis
Induction of swollen vesicle phenotype in mouse NIH3T3 cells incubated for 120 mins by time-lapse analysis
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[PMID: 18188180] |
Acute treatment of cells with YM-201636 shows that the PIKfyve pathway is involved in the sorting of endosomal transport, with inhibition leading to the accumulation of a late endosomal compartment and blockade of retroviral exit. The yeast orthologue of PIKfyve, Fab1, is found to be insensitive to YM-201636 (IC50>5 μM). YM-201636 does not inhibit a type IIγ PtdInsP kinase even at 10 μM and inhibits a mouse type Iα PtdInsP kinase with an IC50>2 μM[1]. YM-201636 almost completely inhibits basal and insulin-activated 2-deoxyglucose uptake at doses as low as 160 nM, with IC50=54 nM for the net insulin response. YM-201636 also completely inhibits insulin-dependent activation of class IA PI 3-kinase[2]. At low doses (10-25 nM), YM-201636 inhibits preferentially PtdIns5P rather than PtdIns(3,5)P2 production, whereas at higher doses, the two products are similarly inhibited. YM-201636 at 160 nM inhibits PtdIns5P synthesis twice more effectively compared with PtdIns(3,5)P2 synthesis[3]. MDCK cells treated with YM-201636 accumulate the tight junction protein claudin-1 intracellularly. YM-201636 treatment blocks the continuous recycling of claudin-1/claudin-2 and delays epithelial barrier formation[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 371942-69-7
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Appearance Solid
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Molecular Weight 467.48
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Formel C25H21N7O3
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Color Light yellow to khaki
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SMILES
O=C(NC1=CC=CC(C2=NC(N3CCOCC3)=C4OC5=NC=CC=C5C4=N2)=C1)C6=CC=C(N=C6)N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (16)
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Journal Impact Factor
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Most Recent
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Nat Commun
A gain-of-function TPC2 variant R210C increases affinity to PI(3,5)P2 and causes lysosome acidification and hypopigmentation. [Abstract]2023 Jan 14;14(1):226. PMID: 36641477 -
Nat Commun
Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV. [Abstract]2020 Mar 27;11(1):1620. PMID: 32221306 -
eGastroenterology
2026 Mar 31;4(1):e100348. PMID: 41948149 -
Ecotoxicol Environ Saf
Cadmium induces endosomal/lysosomal enlargement and blocks autophagy flux in rat hepatocytes by damaging microtubules. [Abstract]2021 Nov 19:228:112993. PMID: 34808507 -
J Thromb Haemost
Vps34 derived phosphatidylinositol 3-monophosphate modulates megakaryocyte maturation and proplatelet production through late endosomes/lysosomes. [Abstract]2020 Jul;18(7):1756-1772. PMID: 32056354
YM-201636 purchased from MedChemExpress. Usage Cited in: J Thromb Haemost. 2020 Jul;18(7):1756-1772. [Abstract]
FL MKs isolated over BSA step-gradient on day 3 are treated with indicated concentrations of YM201636 for 18h, and number of proplatelets is counted. Graph shows percentage of MKs forming proplatelets.
YM-201636 purchased from MedChemExpress. Usage Cited in: J Thromb Haemost. 2020 Jul;18(7):1756-1772. [Abstract]
Representative images show proplatelets from control (DMSO) and YM201636 treated MKs (1 µM, 18h). In total, at least 100 MKs forming proplatelets are counted in each experiment and at least 20 cells are analyzed by immunostaining per condition and per experiment (3 independent experiments)
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Molecules
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]2020 Apr 23;25(8):1980. PMID: 32340370 -
PLoS Pathog
2025 Aug 4;21(8):e1013342. PMID: 40758737 -
PLoS Pathog
2025 Jan 2;21(1):e1012800. PMID: 39746094 -
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J Virol
White Spot Syndrome Virus Benefits from Endosomal Trafficking, Substantially Facilitated by a Valosin-Containing Protein, To Escape Autophagic Elimination and Propagate in the Crustacean Cherax quadricarinatus. [Abstract]2020 Nov 23;94(24):e01570-20. PMID: 32967962 -
J Med Virol
2023 Feb;95(2):e28527. PMID: 36695658 -
BMC Immunol
miR32-5p promoted vascular smooth muscle cell calcification by upregulating TNFα in the microenvironment. [Abstract]2020 Jan 17;21(1):3. PMID: 31952480
YM-201636 purchased from MedChemExpress. Usage Cited in: BMC Immunol. 2020 Jan 17;21(1):3. [Abstract]
The influence of PIKfyve for TNFɑ production in BV2 cells by qRT-PCR and Dot-ELISA analysis. a The expression changes of PIKfyve after treated with YM201636 by qRT-PCR analysis. b The expression changes of TNFɑ after treated with YM201636 by qRT-PCR analysis. c The expression changes of TNFɑ after treated with YM201636 by Dot-ELISA analysis. d The gray value analysis for Dot-ELISA. Bars represent mean ± S.D. (n ≥ 3).
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Biochem Biophys Res Commun
PIKFYVE deficiency induces vacuole-like cataract via perturbing late endosome homeostasis. [Abstract]2025 Feb 2:747:151123. PMID: 39778216 -
Asian Pac J Allergy Immunol
Pyroptosis induced by TLR9 ligand, ODN1826, requires ROS production and caspase-11 activation in Raw264.7 cells. [Abstract]2023 Jun 11. PMID: 37302095 -
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Res Sq
2023 Aug 30:rs.3.rs-3154465. PMID: 37693580
Lösungsmittel & Löslichkeit
DMSO : ≥ 47 mg/mL (100.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.35 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Following 3T3L1 adipocyte serum-starvation and insulin stimulation, cell lysates containing protease inhibitors are clarified and then subjected to immunoprecipitation with anti-PIKfyve antibodies. Washed beads are mixed with 100 μM PtdIns and preincubated for 15 min with YM-201636 (100 nM) or vehicle in the assay buffer (50 mM Tris-HCl, pH 7.5, 1 mM EGTA and 10 mM MgCl2). The kinase assay (50 μL final volume) is carried out for 15 min at 37 °C with 15 μM ATP and [γ-32P]ATP (30 μCi). Lipids are extracted, spotted on TLC glass plates (250 μm), resolved by a chloroform/methanol/water/ammonia solvent system and detected by autoradiography[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[2]. Ikonomov OC, et al. YM-201636, 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 May 8;382(3):566-70. [Content Brief]
[3]. Sbrissa D, et al. Functional dissociation between PIKfyve-synthesized PtdIns5P and PtdIns(3,5)P2 by means of the PIKfyve inhibitor YM-201636. Am J Physiol Cell Physiol. 2012 Aug 15;303(4):C436-46. [Content Brief]
[4]. Dukes JD, et al. The PIKfyve inhibitor YM-201636 blocks the continuous recycling of the tight junction proteins claudin-1 and claudin-2 in MDCK cells. PLoS One. 2012;7(3):e28659. [Content Brief]
[5]. 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 May 8;382(3):566-70. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1391 mL | 10.6956 mL | 21.3913 mL | 53.4782 mL |
| 5 mM | 0.4278 mL | 2.1391 mL | 4.2783 mL | 10.6956 mL | |
| 10 mM | 0.2139 mL | 1.0696 mL | 2.1391 mL | 5.3478 mL | |
| 15 mM | 0.1426 mL | 0.7130 mL | 1.4261 mL | 3.5652 mL | |
| 20 mM | 0.1070 mL | 0.5348 mL | 1.0696 mL | 2.6739 mL | |
| 25 mM | 0.0856 mL | 0.4278 mL | 0.8557 mL | 2.1391 mL | |
| 30 mM | 0.0713 mL | 0.3565 mL | 0.7130 mL | 1.7826 mL | |
| 40 mM | 0.0535 mL | 0.2674 mL | 0.5348 mL | 1.3370 mL | |
| 50 mM | 0.0428 mL | 0.2139 mL | 0.4278 mL | 1.0696 mL | |
| 60 mM | 0.0357 mL | 0.1783 mL | 0.3565 mL | 0.8913 mL | |
| 80 mM | 0.0267 mL | 0.1337 mL | 0.2674 mL | 0.6685 mL | |
| 100 mM | 0.0214 mL | 0.1070 mL | 0.2139 mL | 0.5348 mL |
YM-201636 Related Classifications
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