1. PI3K/Akt/mTOR
    Autophagy
  2. PIKfyve
    Autophagy
    PI3K

YM-201636 

Cat. No.: HY-13228 Purity: 98.88%
Data Sheet SDS Handling Instructions

YM-201636 is a potent and selective PIKfyve inhibitor with an IC50 of 33 nM. YM-201636 also inhibits p110α with IC50 of 3.3 μM.

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $98 In-stock
2 mg $55 In-stock
5 mg $95 In-stock
10 mg $170 In-stock
50 mg $640 In-stock
100 mg $1100 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

YM-201636 is a potent and selective PIKfyve inhibitor with an IC50 of 33 nM. YM-201636 also inhibits p110α with IC50 of 3.3 μM.

IC50 & Target

IC50: 33 nM (PIKfyve), 3.3 μM (p110α)[1]

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].

References
Preparing Stock Solutions
Concentration Volume 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.
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
Molecular Weight

467.48

Formula

C₂₅H₂₁N₇O₃

CAS No.

371942-69-7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 47 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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YM-201636
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HY-13228
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