Cat. No.: HY-13228

YM-201636

16 Cited Publications

Customer Review

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.

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

Purity: 98.07%
CAS No.: 371942-69-7
Formula: C₂₅H₂₁N₇O₃
Molecular Weight:467.48

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

YM-201636 Chemical Structure

CAS No.: 371942-69-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (16)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

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

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
NIH3T3	EC₅₀	400 nM Compound: YM201636	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	[PMID: 18188180]

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.

Chemical Information

CAS No. 371942-69-7
Appearance Solid
Molecular Weight 467.48
Formula C₂₅H₂₁N₇O₃
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

Publications (16)

All RT-PCRIF

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Journal Impact Factor

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

Phosphoinositide kinase PIKfyve inhibitor apilimod blocks hepatitis E virus infection. [Abstract]

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)
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

Two-pore channels in MR1-dependent presentation of Mycobacterium tuberculosis infection. [Abstract]

2025 Aug 4;21(8):e1013342. PMID: 40758737
PLoS Pathog

Manganese is a potent inducer of lysosomal activity that inhibits de novo HBV infection. [Abstract]

2025 Jan 2;21(1):e1012800. PMID: 39746094
J Biol Chem

2024 Jun 03.
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

Inhibition of PIKFYVE kinase interferes ESCRT pathway to suppress RNA virus replication. [Abstract]

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).
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
bioRxiv

2023 Aug 12.
Res Sq

Calcium Signaling in MR1-Dependent Antigen Presentation of Mycobacterium tuberculosis. [Abstract]

2023 Aug 30:rs.3.rs-3154465. PMID: 37693580

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protocol

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].

MedChemExpress (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].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Anti-Aging Compound Library Mini

Anti-Infection Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Antiviral Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) YM-201636

All PI3K Isoforms

Biological Activity

Chemical Information

Publications (16)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

YM-201636 Related Classifications

HY-13228 Related Classifications