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YM201636

YM201636 Unit size Cat. code Docs Qty Price
PIKfyve Inhibitor
5 mg
inh-ym20
+-
$182.00

PIKfyve Inhibitor

YM201636 is a potent inhibitor of mammalian phosphatidylinositol phosphate kinase PIP5KIII (PIKfyve) [1]. PIKfyve is the sole enzyme for PtdIns(3,5)P2 biosynthesis that regulates a number of intracellular membrane trafficking pathways [1].

Inhibition of PIKfyve with YM201636 disrupts endomembrane transport and inhibits retroviral release from infected cells [1, 2].

YM201636 can also disrupt glucose homeostasis by halting glucose entry by insulin and inhibiting activation of PI3-kinase [2].

In neurons, YM201636 promotes cell death via a caspase-independent mechanism, and is associated with alterations in autophagy [3]. YM201636 blocks TLR9-signaling by preventing endosomal translocation of CpG-containing oligodeoxynucleotides (CpG ODNs), thus preventing co-localization of agonist and receptor [4].

YM201636 also inhibits TBK-1/IRF3-mediated type I IFN production without affecting NF-kB dependent cytokine production [5].

 

References:

1. Jefferies H. et al., 2008. A selective PIKfyve inhibitor blocks PtdIns(3,5)P(2) production and disrupts endomembrane transport and retroviral budding. EMBO Rep. 2008 Feb;9(2):164-70.
2. Ikonomov O. et al., 2009. YM201636, an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns(3,5)P2 synthesis, halts glucose entry by insulin in adipocytes. BBRC. 382(3):566-70.
3. Martin S. et al., 2013. Inhibition of PIKfyve by YM-201636 dysregulates autophagy and leads to apoptosis-independent neuronal cell death. PLoS One. 8(3):e60152.
4. Hazeki K. et al., 2013. PIKfyve regulates the endosomal localization of CpG oligodeoxynucleotides to elicit TLR9-dependent cellular responses. PLoS One. 8(9):e73894.
5. Kawasaki T. et al., 2013. The second messenger phosphatidylinositol-5-phosphate facilitates antiviral innate immune signaling. Cell Host Microbe. 14(2):148-58.

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Specifications

Working concentration: 0.5- 5 μM

CAS number: 371942-69-7

Synonym: 6- amino- N- [3- [4- (4- morpholinyl)pyrido[3', 2':4, 5]furo[3,2- d]pyrimidin- 2- yl]phenyl]- 3- pyridinecarboxamide

Formula: C25H21N7O3

Molecular weight: 467.5

Solubility: DMSO (20 mg/ml)

Appearance: White powder

Purity: >97% (UHPLC)

Quality control:

  • The absence of bacterial contamination (e.g. endotoxins and peptidoglycans) is controlled using HEK-Blue™ TLR2 and HEK-Blue™ TLR4 cells.
  • The inhibitory activity of the product is validated using a cellular assay.
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Contents

YM201636 is provided as a solid.

  • 5 mg YM201636

YM201636 is shipped at room temperature.

Store at -20˚C.

Solid product is stable 1 year at -20°C.

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