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YM201636
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C25H21N7O3
- MW: 467.48
Description
Selective inhibitor of PIKfyve (type III PtdInsP kinase; IC50 value 33 nM) that blocks PtdIns(3,5)P2 production and disrupts endomembrane transport and retroviral budding and nearly 100-fold selective over p110α. However, YM201636 arrests basal and insulin-induced glucose influx in cultured adipocytes at low nano-molar concentrations (doses are significantly lower than the effective antiretroviral dose), likely by affecting a PIKfyve-unrelated target. Moreover, YM-201636 dysregulates autophagy and promotes neuronal cell death in primary hippocampal neurons in culture.
More Information
| Parent CAS No. | 371942-69-7 |
|---|---|
| Chemical Name | 6-Amino-N-[3-(6-morpholin-4-yl-8-oxa-3,5,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaen-4-yl)phenyl]pyridine-3-carboxamide |
| SMILES | C1=NC(N)=CC=C1C(NC1=CC=CC(C2=NC(N3CCOCC3)=C3OC4=NC=CC=C4C3=N2)=C1)=O |
| MFCD | N.A. |
| InChi | InChI=1S/C25H21N7O3/c26-19-7-6-16(14-28-19)24(33)29-17-4-1-3-15(13-17)22-30-20-18-5-2-8-27-25(18)35-21(20)23(31-22)32-9-11-34-12-10-32/h1-8,13-14H,9-12H2,(H2,26,28)(H,29,33) |
| InChiKey | YBPIBGNBHHGLEB-UHFFFAOYSA-N |
| CID | 9956222 |
| Short Description | PIKfyve inhibitor |
References
- HB Jefferies et al. 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.
- OC Ikonomov 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 May 8;382(3):566-70.
- S Martin et al. Inhibition of PIKfyve by YM-201636 dysregulates autophagy and leads to apoptosis-independent neuronal cell death. PLoS One. 2013;8(3):e60152.
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