YM-201636

SKU: orb1301064

Description

YM201636 is a potent and selective PIKfyve inhibitor with an IC50 of 33 nM. It exhibits minimal activity against p110α and no effect on the yeast orthologue Fab1. This compound is a valuable research tool for studying lysosomal function and autophagy in cellular and animal models of related diseases.

Research Area

Cell Biology, Infectious Disease & Virology, Signal Transduction

Key Properties

• CAS Number: 371942-69-7
• MW: 467.48
• Purity: 98.30% (May vary between batches)
• Formula: C₂₅H₂₁N₇O₃
• SMILES: Cl.Nc1ccc(cn1)C(=O)Nc1cccc(c1)-c1nc(N2CCOCC2)c2oc3ncccc3c2n1
• Target: Autophagy,Influenza Virus,PI3K
• Solubility: DMSO:13.33 mg/mL (28.51 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.28 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  p110α:3.3 μM|PIKfyve:33 nM
• In Vivo:
  In NIH3T3 cells treated with serum starvation, YM201636 (0.8 μM) significantly reduces the production of PtdIns(3,5)P2 by up to 80%. In 3T3-L1 adipocytes, YM-201636 (IC50=54 nM) inhibits the absorption of 2-deoxyglucose, and at a dose of 160 nM, it fully inhibits the absorption of 2-deoxyglucose. In MDCK cells, YM201636 disrupts the continuous recycling of the intercellular junction proteins Claudin-1 and Claudin-2, leading to their accumulation within the cells and delaying the formation of epithelial barriers.
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• Cell Research:
  YM-201636 is dissolved in DMSO and diluted with DMEM and added to cells at a final concentration of 800 nM. Cells are treated with YM-201636 or a DMSO control for 2 h. For TER measurements cells are plated at confluency on Transwell permeable polyester filters (0.4 μM pore size) with surface area of 0.33 cm2. Media is changed ever 2-3 days and cells are grown for 7 days prior to TER measurements.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

p110α, Inhibitor, Influenza Virus, InfluenzaVirus, inhibit, Fab1, Autophagy, Phosphoinositide 3-kinase, PIKfyve, PI3K, YM201636, YM-201636, YM 201636

Compound Identifiers

PubChem CID

91895221