YM201636

Catalog No.S1219

YM201636 Chemical Structure

Molecular Weight(MW): 467.48

YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue).

Size Price Stock Quantity  
In DMSO USD 320 In stock
USD 170 In stock
USD 270 In stock
USD 570 In stock
USD 870 In stock
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1 Customer Review

  • 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).
Targets
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]

Protocol

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 467.48
Formula

C25H21N7O3

CAS No. 371942-69-7
Storage powder
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID