YM201636

YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM.

Catalog No.S1219
Price Stock Quantity  
USD 170 In stock
USD 270 In stock
USD 570 In stock
USD 870 In stock

Free Overnight Delivery on all orders over $ 500.

Order now and get it on

YM201636 Chemical Structure
Molecular Weight: 467.48

Related Compound Libraries

Product Information

  • Compare PI3K Inhibitors
    Compare PI3K Inhibitors
  • Research Area

Product Description

Biological Activity

Description YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM.
Targets PIKfyve
IC50 33 nM [1]
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]
In vivo
Clinical Trials
Features

Protocol(Only for Reference)

Kinase Assay: [1]

In vitro GST-PIKfyve assay The assay is performed in kinase buffer (25 mM HEPES pH 7.4, 120 mM NaCl, 1.5 mM MgCl2, 5 mM 2-glycerophosphate, and 1 mM DTT) containing 100 μM PI(3)P, GST-PIKfyve, 50 μM ATP/10 μCi [32P]γATP and increasing concentrations of YM201636 in a final volume of 65 μL. The reactions are incubated for 15 minutes at 30 °C, and stopped by the addition of 243 μL of 2:1 MeOH : CHCl3 (volume : volume). Lipid products labelled with 32P are analysed by thin-layer chromatography and quantified by Cerenkov counting. IC50 value is determined by using Graphpad Prism and errors are given as ±95% confidence limit.
1

References

Chemical Information

Download YM201636 SDF
Molecular Weight (MW) 467.48
Formula

C25H21N7O3

CAS No. 371942-69-7, 371933-96-9 (2HCl)
Synonyms N/A
Storage 2 years -20°CPowder
2 weeks4°Cin DMSO
6 months-80°Cin DMSO
Chemical Name 3-Pyridinecarboxamide, 6-amino-N-[3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenyl]-

Research Area

Tech Support & FAQs

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.

Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related PI3K Inhibitors

  • BEZ235 (NVP-BEZ235)

    BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively, and also inhibits ATR with IC50 of 21 nM.

  • PI-103

    PI-103 is a potent, ATP-competitive PI3K inhibitor of DNA-PK, p110α, mTORC1, PI3KC2β, p110δ, mTORC2, p110β, and p110γ with IC50 of 2 nM, 8 nM, 20 nM, 26 nM, 48 nM, 83 nM, 88 nM and 150 nM, respectively.

  • GDC-0941

    GDC-0941 is a potent inhibitor of PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ with IC50 of 3 nM, 33 nM, 3 nM and 75 nM, respectively.

  • ZSTK474

    ZSTK474 is a potent pan-class I PI3K inhibitor with IC50 of 37 nM.

  • LY294002

    LY294002 is a PI3K inhibitor for p110α, p110δ and p110β with IC50 of 0.5 μM, 0.57 μM and 0.97 μM, respectively.

  • XL147

    XL147 (SAR245408) is a selective and reversible class I PI3K inhibitor for wild type and mutant p110α with IC50 of 40 nM and 40 nM, respectively.

  • TGX-221

    TGX-221 is a potent, selective PI3K inhibitor for p110β with IC50 of 8.5 nM.

  • PIK-90

    PIK-90 is a potent and cell permeable inhibitor of p110α, p110β, p110γ and p110δ with IC50 of 11 nM, 350 nM, 18 nM and 58 nM, respectively.

  • PIK-75

    PIK-75 is a selective and competitive inhibitor of p110α with IC50 of 5.8 nM and also potently inhibits DNA-PK with IC50 of 2 nM.

  • IC-87114

    IC-87114 is a selective inhibitor of PI3Kδ with IC50 of 0.5 μM.

Recently Viewed Items

Tags: buy YM201636 | YM201636 supplier | purchase YM201636 | YM201636 cost | YM201636 manufacturer | order YM201636 | YM201636 distributor
Contact Us