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

YM-201636 

Cat. No.: HY-13228 Purity: 98.22%
Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 117 In-stock
Estimated Time of Arrival: December 31
2 mg USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 114 In-stock
Estimated Time of Arrival: December 31
10 mg USD 204 In-stock
Estimated Time of Arrival: December 31
50 mg USD 768 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    YM-201636 purchased from MCE. Usage Cited in: BMC Immunol. 2020 Jan 17;21(1):3. 

    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).

    YM-201636 purchased from MCE. Usage Cited in: J Thromb Haemost. 2020 Feb 13. 

    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 MCE. Usage Cited in: J Thromb Haemost. 2020 Feb 13. 

    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)
    • Biological Activity

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    • 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].

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

    Molecular Weight

    467.48

    Formula

    C₂₅H₂₁N₇O₃

    CAS No.

    371942-69-7

    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 47 mg/mL (100.54 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" 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
    10 mM 0.2139 mL 1.0696 mL 2.1391 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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
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    Keywords:

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

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