For research use only.

Catalog No.S1219

6 publications

YM201636 Chemical Structure

CAS No. 371942-69-7

YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction of autophagy.

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Selleck's YM201636 has been cited by 6 publications

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  • Validation study for vacuolin-1 and YM201636. (A) HeLa cells were treated with 3 lM vacuolin-1 or YM201636 in the presence or absence of the lysosomal protease inhibitor E64d (10 μg/mL) and pepstatin A (10 μg/mL). After 24 h of treatment, cell lysates (10 μg) were separated by 10% polyacrylamide gel electrophoresis, and LC3 was detected via immunoblotting.

    FEBS Letters, 2016, 590:1576-1585.. YM201636 purchased from Selleck.

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Biological Activity

Description YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction of autophagy.
PIKfyve [1]
(Cell-free assay)
p110α [1]
(Cell-free assay)
33 nM 3.3 μM
In vitro

YM201636 potently inhibits mammalian PIKfyve with an IC50 of 33 nM but not yeast orthologue Fab1 with an IC50 of >5 μM, exhibiting around 100-fold selectivity for PtdIns3P p110α with an IC50 of 3 μM. YM201636 (0.8 μM) significantly decreases the production of PtdIns(3,5)P2 by 80% in serum-starved NIH3T3 cells followed by serum stimulation with no effect on serum-stimulated protein kinase B (PKB) Ser 473 phosphorylation. YM-201636 reversibly impairs endosomal trafficking in NIH3T3 cells by blocking PIKfyve and PtdIns(3,5)P2 production, mimicking the effect produced by depleting PIKfyve with siRNA. YM-201636 (0.8 μM) also significantly reduces retroviruses budding from cells by 80%, apparently through interfering with the endosomal sorting complex required for transport (ESCRT) machinery. [1] In 3T3L1 adipocytes, YM-201636 inhibits basal and insulin-activated 2-deoxyglucose uptake with an IC50 of 54 nM, with almost complete inhibition at doses as low as 160 nM. YM-201636 (0.1 μM) has also been shown to completely block insulin-dependent activation of class IA PI 3-kinase. [2] Although not involved in NPM-ALK-dependent proliferation and migration, YM201636 (0.4 μM) strongly reduces invasive capacities of NPM-ALK-expressing cells and their capacity to degrade the extracellular matrix. [3] YM201636 treatment blocks the continuous recycling of junctional proteins claudin-1 and claudin-2 in MDCK cells, leading to the intracellular accumulation and delay of epithelial barrier formation. [4]


Solubility (25°C)

In vitro DMSO 35 mg/mL (74.86 mM)
Water Insoluble
Ethanol Insoluble

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Chemical Information

Molecular Weight 467.48


CAS No. 371942-69-7
Storage powder
in solvent
Synonyms N/A
Smiles C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)NC(=O)C6=CN=C(C=C6)N

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID