YM201636 Inhibitor CAS No. 371942-69-7

Cat. No.	Name	Size	Price
KI2014	YM201636	5 mg	$272
	YM201636	10 mg	$432
	YM201636	50 mg	$1392
	YM201636	200 mg	$4200

Chemical Characteristic

Product Name	YM201636
CAS No.	371942-69-7
Molecular Weight	467.48
Formula	C₂₅H₂₁N₇O₃
Chemical Name	6-Amino-N-[3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenyl]-3-pyridinecarboxamide
Smiles	c1c(ccc(n1)N)C(=O)Nc1cc(ccc1)c1nc2c(c(n1)N1CCOCC1)oc1c2cccn1
Chemical Structure

Biological activities

YM201636 is a selective PIKfyve inhibitor. YM201636 inhibits mammalian class III phosphatidylinositol phosphate kinase PIKfyve enzymatic activity with an IC50 of 33 nM. YM201636 also inhibits PtdIns3P p110a with an IC50 of 3 µM.^[1] YM201636 (0-4 mM) induces a marked inhibition of both basal and insulin-activated 2DG uptake in a dose-dependent manner. YM201636 completely inhibits basal and insulin-activated 2-deoxyglucose uptake at doses as low as 160 nM, with an IC50 of 54 nM for the net insulin response. In addition to PIKfyve, YM201636 (100 nM) completely inhibits insulin-dependent activation of class IA PI3-kinase.^[2] YM201636 inhibits the constant recycling of claudin-1 and causes it to accumulate intracellularly. Addition of YM201636 blocks the continuous recycling of claudin-1 and claudin-2 and delays barrier formation in epithelial cells.^[3] Besides, YM201636 significantly reduces the survival of primary mouse hippocampal neurons in culture. Accordingly, YM201636 increases the level of the autophagosomal marker protein LC3-II in mouse.^[4]

Protocols

In vitro, YM201636 is dissolved in DMSO.^[2]

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. [2] 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, 382(3): 566-570. [3] Dukes JD, et al. The PIKfyve inhibitor YM201636 blocks the continuous recycling of the tight junction proteins claudin-1 and claudin-2 in MDCK cells. PLoS One. 2012, 7(3): e28659. [4] Martin S, et al. Inhibition of PIKfyve by YM-201636 dysregulates autophagy and leads to apoptosis-independent neuronal cell death. PLoS One. 2013, 8(3): e60152.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com