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YM201636

Cat. No. M3304
YM201636 Structure
Size Price Availability Quantity
5mg USD 140 In stock
10mg USD 220 In stock
50mg USD 690 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

YM201636 is a novel PIKfyve-specific inhibitor with an IC50 of 54 nM for the net insulin response. YM201636 disrupts retroviral budding. Treatment of a Moloney leukemia virus-expressing cell line with YM201636 (800 nM) inhibits retroviral release by 80%. YM201636 (0-4 μM) significantly inhibits both basal and insulin-activated 2DG uptake in a dose-dependent manner. At concentrations as low as 160 nM, YM201636 nearly completely prevents the net insulin effect. A YM201636 concentration as high as 800 nM inhibits cell surface HA-GLUT4-eGFP accumulation by 45%. YM201636 at the concentration of 800 nM leads to a 55% inhibition of Akt-Ser473 phosphorylation and no detectable changes in total Akt. YM201636 also inhibits the insulin-dependent class IA PI 3-kinase activation at nanomolar doses. YM201636 blocks the endocytic recycling of claudin-1, providing an explanation for the intracellular accumulation. Claudin-2 is also found to constantly recycle in confluent MDCK cells and treatment with YM201636 prevents this recycling and caused accumulation of intracellular claudin-2.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 467.48
Formula C25H21N7O3
CAS Number 371942-69-7
Purity >98%
Solubility DMSO 30 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: YM201636 supplier, PI3K, inhibitors

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