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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

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About This Item

Empirical Formula (Hill Notation):
C25H21N7O3
CAS Number:
371942-69-7
Molecular Weight:
467.48
MDL number:
MFCD16038303
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

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

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)

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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