KU-0063794 Inhibitor CAS No. 938440-64-3

Cat. No.	Name	Size	Price
KI1371	KU-0063794	5 mg	$144
	KU-0063794	25 mg	$330
	KU-0063794	50 mg	$550
	KU-0063794	100 mg	$870

Chemical Characteristic

Product Name	KU-0063794
CAS No.	938440-64-3
Molecular Weight	465.54
Formula	C₂₅H₃₁N₅O₄
Chemical Name	[5-[2-[(2R,6S)-2,6-dimethylmorpholin-4-yl]-4-morpholin-4-ylpyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol
Smiles	c1(c(ccc(c1)c1ccc2c(nc(nc2N2CCOCC2)N2C[C@H](O[C@H](C2)C)C)n1)OC)CO
Chemical Structure

Biological activities

Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Ku-0063794 inhibits mTORC1 with an IC50 of ∼10 nM, as well as mTORC2. Ku-0063794 prevents phosphorylation of the T-loop Thr³⁰⁸ residue of Akt phosphorylated by PDK1 (3-phosphoinositide-dependent protein kinase-1). Ku-0063794 induces a much greater dephosphorylation of the mTORC1 substrate 4E-BP1 (eukaryotic initiation factor 4E-binding protein 1) than rapamycin, even in mTORC2-deficient cells. Ku-0063794 suppresses cell growth and induces a G1-cell-cycle arrest. Ku-0063794 prevents phosphorylation of the T-loop residue (Thr²²⁹). Ku-0063794 also inhibits phosphorylation of the ribosomal S6 protein, an S6K substrate. Ku-0063794 inhibits mTORC2 activity in HEK-293 cells. Ku-0063794 inhibits NDRG1 phosphorylation to the same extent as it prevents SGK1 activity. In addition, Ku-0063794 induces complete dephosphorylation of 4E-BP1. Ku-0063794 also suppresses cell growth and induces G1-cell cycle arrest off mLST8-fibroblast cell lines.^[1]

Protocols

Molecular levels: HEK-293 cells are freshly lysed in Hepes lysis buffer. Lysate (1?? mg) is pre-cleared by incubating with 5??0 µL of Protein G??epharose conjugated to pre-immune IgG. The lysate extracts are then incubated with 5??0 µL of Protein G??epharose conjugated to 5??0 µg of either anti-Rictor or anti-Raptor antibody, or pre-immune IgG. All antibodies are covalently conjugated to Protein G??epharose. Immunoprecipitations are carried out for 1 hour at 4 °C on a vibrating platform. The immunoprecipitates are washed four times with Hepes lysis buffer, followed by two ishes with Hepes kinase buffer. For Raptor immunoprecipitates used for phosphorylating S6K1, for the initial two ish steps the buffer included 0.5 M NaCl to ensure optimal kinase activity. GST??kt1 is isolated from serum-deprived HEK-293 cells incubated with PI-103 (1 µM for 1 hour). GST??6K1 is purified from serum-deprived HEK-293 cells incubated with rapamycin (0.1 µM for 1 hour). mTOR reactions are initiated by adding 0.1 mM ATP and 1 mM MgCl_{2 in the presence or absence of Ku- 63794 and GST??kt1 (0.5 µg) or GST??6K1 (0.5 µg). Reaction are carried out for 3 minutes at 30°C on a vibrating platform and stopped by addition of SDS sample buffer. Reaction mixtures are then filtered through a 0.22-µm-pore-size Spin-X filter and samples are subjected to electrophoresis and immunoblot analysis.^[1]}

References

[1] Garc?a-Mart?nez JM, et al. Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem J. 2009 , 421(1): 29-42.

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