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HomeProduct name listKU-0063794

KU-0063794

Synonym(s):mTOR Inhibitor IV, Ku-63794 - CAS 938440-64-3 - Calbiochem;rel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morp holinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol;rel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol, Ku-0063794, mTOR Inhibitor IV, Ku-63794

KU-0063794 Structural

What is KU-0063794?

Description

The mammalian target of rapamycin (mTOR) is a serine-threonine kinase which acts as part of two distinct complexes, TORC1 and TORC2. Both complexes (TORC1/2) play central roles in cell growth, gene expression, angiogenesis, and cell survival. Ku-0063794 is a cell-permeable, selective dual inhibitor of mTORC1 and mTORC2 (IC50 = 10 nM). It does not affect the activity of 76 other protein kinases or seven lipid kinases, including PI3Ks. Ku-0063794 inhibits cell growth by inducing G1-cell cycle arrest and autophagy, but not apoptosis, and inhibits tumor growth in a xenograft model of renal cell carcinoma (8 mg/kg for 46 days).

The Uses of KU-0063794

Ku 0063794 is a specific mammalian target of rapamycin (mTOR) inhibitor and may be used for the treatment of cancers.

The Uses of KU-0063794

KU 0063794 has been used:

  • as a mammalian target of rapamycin (mTOR) inhibitor to study the effects of follicular stimulating hormone (FSH) in mTOR phosphorylation and vascular cell adhesion molecule-1 (VCAM-1) expression in?human umbilical vascular endothelial cells (HUVECs)
  • as a mTOR inhibitor to treat effector memory (EM) CD8+ T cells for metabolic flux analysis
  • as an autophagy inducer to demonstrate the utility of p62 and LC3B-II quantification in HEK293T cells and primary cultures of rat neurons and astrocytes using time-resolved fluorescence resonance energy transfer (TR-FRET)

What are the applications of Application

KU 0063794 is a FRAP (mTOR) inhibitor for both mTORC1 and mTORC2

Definition

ChEBI: A member of the class of pyridopyrimidines that is an mTOR inhibitor and shows anti-tumour properties.

Biological Activity

Selective inhibitor of mammalian target of rapamycin (mTOR) (IC 50 ~10 nM for mTORC1 and mTORC2 respectively). Displays no activity at PI 3-kinase or 76 other kinases tested. Inhibits activation and hydrophobic motif phosphorylation of Akt, S6K and SGK, but not RSK. Suppresses cell growth and induces G 1 cell cycle arrest in vitro .

Biochem/physiol Actions

KU 0063794 induces autophagy. It is cell-permeant and suppresses activation and hydrophobic motif phosphorylation of protein kinase B (Akt), p70 ribosomal S6 kinase (S6K) and serum and glucocorticoid protein kinase (SGK).

storage

Room temperature

Properties of KU-0063794

Boiling point: 694.3±65.0 °C(Predicted)
Density  1.248
storage temp.  2-8°C
solubility  DMSO: >2mg/mL (warmed)
pka 14.20±0.10(Predicted)
form  powder
color  white to beige

Safety information for KU-0063794

Computed Descriptors for KU-0063794

InChIKey RFSMUFRPPYDYRD-CALCHBBNSA-N

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