2. PI3K/Akt/mTOR Autophagy Anti-infection
  3. PIKfyve PI3K Autophagy Influenza Virus
  4. YM-201636

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.

For research use only. We do not sell to patients.

YM-201636 Chemical Structure

YM-201636 Chemical Structure

CAS No. : 371942-69-7

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 129 In-stock
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2 mg USD 73 In-stock
5 mg USD 125 In-stock
10 mg USD 224 In-stock
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50 mg USD 845 In-stock
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Customer Review

Based on 15 publication(s) in Google Scholar

YM-201636 Related Antibodies

Top Publications Citing Use of Products

    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)

    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).

    View All PI3K Isoform Specific Products:

    View All Isoforms
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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.

    IC50 & Target[1]

    PIKfyve

    33 nM (IC50)

    p110α

    3.3 μM (IC50)

    Autophagy

     

    In Vitro

    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.

    YM-201636 Related Antibodies
    Molecular Weight

    467.48

    Formula

    C25H21N7O3
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to khaki

    SMILES

    O=C(NC1=CC=CC(C2=NC(N3CCOCC3)=C4OC5=NC=CC=C5C4=N2)=C1)C6=CC=C(N=C6)N
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    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.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation
    References
    Kinase Assay
    [2]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [4]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    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
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    YM-201636 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    YM-201636371942-69-7YM201636YM 201636PIKfyvePI3KAutophagyInfluenza VirusFYVE domain-containing phosphatidylinositol 3-phosphate 5-kinasePhosphatidylinositol 3-phosphate 5-kinaseFab1Phosphoinositide 3-kinaseInhibitorinhibitorinhibit

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