KU-0063794

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Cat No.

CEI-0142

Description

Ku-0063794 can inhibits both mTORC1 and mTORC2 with an IC50 of approximately 10 nM.

CAS_No

938440-64-3

Molecular Weight

465.54

Purity

>99%

Storage

2 years at -20centigrade Powder

Targets

mTORC1, mTORC2

Molecular Formula

C25H31N5O4

Chemical Name

(5-(2-((2R,6S)-2,6-dimethylmorpholino)-4-morpholinopyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol

Solubility

DMSO 16 mg/mL Water

In vitro

Ku-0063794 can inhibits both mTORC1 and mTORC2 with an IC50 of approximately 10 nM without inhibiting the activity of 76 other protein kinases or seven lipid kinases. Ku-0063794 is cell permeant, suppresses activation and hydrophobic motif phosphorylation of Akt, S6K and SGK, but not RSK (ribosomal S6 kinase), an AGC kinase not regulated by mTOR. Ku-0063794 also inhibited phosphorylation of the T-loop Thr308 residue of Akt phosphorylated by PDK1 (3-phosphoinositide-dependent protein kinase-1). Ku-0063794 can induce a much greater dephosphorylation of the mTORC1 substrate 4E-BP1 (eukaryotic initiation factor 4E-binding protein 1) than rapamycin, even in mTORC2-deficient cells, suggesting a form of mTOR distinct from mTORC1, or mTORC2 phosphorylates 4E-BP1. Ku-0063794 also suppressed cell growth and induced a G1-cell-cycle arrest.

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