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Merck

SML0382

KU 0063794

≥98% (HPLC)

Synonym(s):

rel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morp holinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol

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About This Item

Empirical Formula (Hill Notation):
C25H31N5O4
CAS Number:
938440-64-3
Molecular Weight:
465.54
NACRES:
NA.77
PubChem Substance ID:
329825382
UNSPSC Code:
12352200
MDL number:
MFCD11977741

Key Documents

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Product Name

KU 0063794, ≥98% (HPLC)

form

powder

InChI

1S/C25H31N5O4/c1-16-13-30(14-17(2)34-16)25-27-23-20(24(28-25)29-8-10-33-11-9-29)5-6-21(26-23)18-4-7-22(32-3)19(12-18)15-31/h4-7,12,16-17,31H,8-11,13-15H2,1-3H3/t16-,17+

SMILES string

COc1ccc(cc1CO)-c2ccc3c(nc(nc3n2)N4C[C@H](C)O[C@H](C)C4)N5CCOCC5

InChI key

RFSMUFRPPYDYRD-CALCHBBNSA-N

assay

≥98% (HPLC)

color

white to beige

solubility

DMSO: >2 mg/mL (warmed)

storage temp.

2-8°C

Quality Level

100

Related Categories

Application

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)

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).
KU 0063794 is a potent and selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for both mTORC1 and mTORC2) that inhibits both mTORC1 and mTORC2 in vitro and in vivo (IC50 ~10 nM for both mTORC1 and mTORC2). KU 0063794 does not significantly inhibit 76 other protein kinases tested as well as seven lipid kinases including PI3K and AKT.
KU 0063794 is a potent and selective inhibitor of mammalian target of rapamycin (mTOR); inhibits both mTORC1 and mTORC2 in vitro and in vivo.

Features and Benefits

This compound is featured on the PKB/Akt page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000126499
0000126498
0000117621
0000065462
0000065466

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Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR)
Garcaa-Martanez JM, et al.
The Biochemical Journal, 421(1), 29-42 (2009)
Follicular stimulating hormone accelerates atherogenesis by increasing endothelial VCAM-1 expression
Li X, et al.
Theranostics, 7(19), 4671-4671 (2017)
Quantifying autophagy using novel LC3B and p62 TR-FRET assays
Bresciani A, et al.
PLoS ONE, 13(3) (2018)
Juan M García-Martínez et al.
The Biochemical journal, 421(1), 29-42 (2009-05-01)
mTOR (mammalian target of rapamycin) stimulates cell growth by phosphorylating and promoting activation of AGC (protein kinase A/protein kinase G/protein kinase C) family kinases such as Akt (protein kinase B), S6K (p70 ribosomal S6 kinase) and SGK (serum and glucocorticoid
Mitochondria-endoplasmic reticulum contact sites function as immunometabolic hubs that orchestrate the rapid recall response of memory CD8+ T cells
Bantug GR, et al.
Immunity, 48(3), 542-555 (2018)
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