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安全信息

SML0382

Sigma-Aldrich

KU 0063794

≥98% (HPLC)

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别名:
rel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morp holinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol
经验公式（希尔记法）:
C25H31N5O4
CAS号:
938440-64-3
分子量:
465.54
MDL编号:
MFCD11977741
UNSPSC代码:
12352200
PubChem化学物质编号:
329825382
NACRES:
NA.77

质量水平

100

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: >2 mg/mL (warmed)

储存温度

2-8°C

SMILES字符串

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

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+

InChI key

RFSMUFRPPYDYRD-CALCHBBNSA-N

应用

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)

生化/生理作用

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.

特点和优势

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.

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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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
Quantifying autophagy using novel LC3B and p62 TR-FRET assays
Bresciani A, et al.
Testing, 13(3) (2018)
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