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YM201636

YM201636

Item no.	S1219-5
Manufacturer	Selleckchem
CASRN	371942-69-7
Amount	5 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 mL 25 mg 5 mg 50 mg 5 g
Category	Neuroscience Metabolism Diabetes Cholesterol & Lipid Metabolism Regulation of Appetite Molecular Targets for Neuroscience Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Smiles	C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)NC(=O)C6=CN=C(C=C6)N
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	371942-69-7'
Similar products	YM201636
Available
Manufacturer - Targets	PI3K
Storage Conditions	2 years -80 in solvent
Molecular Weight	467, 48
IC50	33 nM [1], 33 nM [1], 33 nM [1], 33 nM [1], 33 nM [1], 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 uM, exhibiting around 100-fold selectivity for PtdIns3P p110alpha with an IC50 of 3 uM. YM201636 (0.8 uM) 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 uM) 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 uM) 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 uM) 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]
Kinase Assay	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 uM PI(3)P, GST-PIKfyve, 50 uM ATP/10 uCi [32P]gammaATP and increasing concentrations of YM201636 in a final volume of 65 uL. The reactions are incubated for 15 minutes at 30 C, and stopped by the addition of 243 uL 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.
Solubility (25C)	DMSO 35 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction of autophagy.
Chemical Name	3-Pyridinecarboxamide, 6-amino-N-[3-[4-(4-morpholinyl)pyrido[3', 2':4, 5]furo[3, 2-d]pyrimidin-2-yl]phenyl]-

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