524611-M

PIKfyve Inhibitor

The PIKfyve Inhibitor, also referenced under CAS 371942-69-7, controls the biological activity of PIKfyve. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): PIKfyve Inhibitor, 6-Amino-N-(3-(4-(4-morpholinyl)pyrido[3ʹ2ʹ:4,5]furo[3,2-d]pyrimidin-2-yl)phenyl)-3-pyridine carboxamide, PtdIns3P 5-KInase Inhibitor, YM201636
• Empirical Formula (Hill Notation): C₂₅H₂₁N₇O₃
• CAS Number: 371942-69-7
• Molecular Weight: 467.48
• MDL number: MFCD16038303
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 1 mg/mL
• storage temp.: −20°C
• SMILES string: N6(CCOCC6)c1nc(nc4c1[o]c5ncccc54)c2cc(ccc2)NC(=O)c3cnc(cc3)N
• 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)
• InChI key: YBPIBGNBHHGLEB-UHFFFAOYSA-N

Description

General description

A cell-permeable pyridofuropyrimidine compound that selectively inhibits mammalian type III PtdInsP kinase (IC₅₀ = 33 nM and >5 µM using murine PIKfyve and yeast Fab1, respectively), while exhibiting much reduced activity against p110α (IC₅₀ = 3.3 µM) and little activity against type IIγ PtdInsP kinase even at concentrations as high as 10 µM. Shown to block serum-induced PtdIns(3,5)P₂ production in NIH3T3 cells (80% inhibition at 800 nM) and disrupt cellular endosomal transport in a reversible manner.

Preparation Note

Enhanced solubility in DMSO can be achieved by the addition of a small drop of TFA.

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Jefferies, H.B.J., et al. 2008. EMBO Reports9, 164.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable