Art. -Nr.: HY-50710

KU-0063794

15 Cited Publications

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Based on 15 publication(s) in Google Scholar

KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC₅₀s of 10 nM.

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Reinheit: 99.67%
CAS. Nr.: 938440-64-3
Formel: C₂₅H₃₁N₅O₄
Molecular Weight:465.54

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

KU-0063794 Chemical Structure

CAS. Nr.: 938440-64-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (15)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC₅₀s of 10 nM.

IC₅₀ & Target^[1]

mTORC1

10 nM (IC₅₀)

mTORC2

10 nM (IC₅₀)

Alle mTOR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.0025 μM Compound: Ku-0063794	Inhibition of recombinant FLAG-tagged mTOR (1362 to 2549) (unknown origin) expressed in HEK293 cells Inhibition of recombinant FLAG-tagged mTOR (1362 to 2549) (unknown origin) expressed in HEK293 cells	[PMID: 23375793]
HEK293	IC₅₀	0.003 μM Compound: 31	Inhibition of recombinant FLAG-tagged mTOR expressed in HEK293 cells using biotinylated p70S6K substrate after 2 hrs by alphascreen competition assay Inhibition of recombinant FLAG-tagged mTOR expressed in HEK293 cells using biotinylated p70S6K substrate after 2 hrs by alphascreen competition assay	[PMID: 19762236]
HEK293	IC₅₀	10 nM Compound: 16; Ku-0063794	Inhibition of mTORC1 in HEK293 cells using GST-tagged S6K1 or Akt1 as substrate after 30 mins by immunoblotting assay Inhibition of mTORC1 in HEK293 cells using GST-tagged S6K1 or Akt1 as substrate after 30 mins by immunoblotting assay	[PMID: 29211480]
HEK293	IC₅₀	10 nM Compound: 16; Ku-0063794	Inhibition of mTORC2 in HEK293 cells using GST-tagged S6K1 or Akt1 as substrate after 30 mins by immunoblotting assay Inhibition of mTORC2 in HEK293 cells using GST-tagged S6K1 or Akt1 as substrate after 30 mins by immunoblotting assay	[PMID: 29211480]
HeLa	IC₅₀	0.016 μM Compound: 31	Inhibition of mTOR in human HeLa cells using 4E-BP1 substrate by ELISA Inhibition of mTOR in human HeLa cells using 4E-BP1 substrate by ELISA	[PMID: 19762236]
MDA-MB-468	IC₅₀	0.24 μM Compound: Ku-0063794	Inhibition of mTORC2 in human MDA-MB-468 cells assessed as reduction of AKT phosphorylation at Ser473 after 2 hrs Inhibition of mTORC2 in human MDA-MB-468 cells assessed as reduction of AKT phosphorylation at Ser473 after 2 hrs	[PMID: 23375793]
MDA-MB-468	IC₅₀	0.66 μM Compound: Ku-0063794	Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction of pS6 phosphorylation at Ser235/236 after 2 hrs Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction of pS6 phosphorylation at Ser235/236 after 2 hrs	[PMID: 23375793]
T47D	GI₅₀	0.35 μM Compound: 31	Antiproliferative activity against human T47D cells after 120 hrs by SRB assay Antiproliferative activity against human T47D cells after 120 hrs by SRB assay	[PMID: 19762236]
U-87MG ATCC	IC₅₀	0.1 μM Compound: 31	Inhibition of mTORC1 in human U87MG cells assessed as phosphorylated S6 ribosomal protein (Ser235/236) level after 2 hrs by Western blotting Inhibition of mTORC1 in human U87MG cells assessed as phosphorylated S6 ribosomal protein (Ser235/236) level after 2 hrs by Western blotting	[PMID: 19762236]
U-87MG ATCC	IC₅₀	0.15 μM Compound: 31	Inhibition of mTORC2 in human U87MG cells assessed as phosphorylated AKT (Ser473) level after 2 hrs by Western blotting Inhibition of mTORC2 in human U87MG cells assessed as phosphorylated AKT (Ser473) level after 2 hrs by Western blotting	[PMID: 19762236]

In Vitro

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 inhibits 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, suggesting a form of mTOR distinct from mTORC1, or mTORC2 phosphorylates 4E-BP1. Ku-0063794 also suppresses cell growth and induced a G1-cell-cycle arrest^[1]. Ku0063794 does not alter nuclear phospho-Mst1-Thr-120 levels in LNCaP cell nuclei, whereas Ku0063794 or CCI-779 increases phospho-Mst1-Thr-120 levels in C4-2 cell nuclei^[2]. The combination of GDC-0941 and KU0063794 inhibits the phosphorylation of 4EBP1 and S6 to a similar extent to that caused by single agent NVP-BEZ235 in HCT116, DLD1 and HT29 cell lines^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 938440-64-3
Appearance Solid
Molecular Weight 465.54
Formel C₂₅H₃₁N₅O₄
Color Light yellow to yellow
SMILES

OCC1=CC(C2=CC=C3C(N=C(N=C3N4CCOCC4)N5C[C@@H](O[C@@H](C5)C)C)=N2)=CC=C1OC
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (15)

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Journal Impact Factor

Cell

Distinct longevity mechanisms across and within species and their association with aging. [Abstract]

2023 Jun 22;186(13):2929-2949.e20. PMID: 37269831
Cell Metab

Identification and Application of Gene Expression Signatures Associated with Lifespan Extension. [Abstract]

2019 Sep 3;30(3):573-593.e8. PMID: 31353263
Gut

DYRK1B blockade promotes tumoricidal macrophage activity in pancreatic cancer. [Abstract]

2024 Jun 4:gutjnl-2023-331854. PMID: 38834297
Neuron

Intrinsic endothelial remodeling drives brain capillary repair. [Abstract]

2026 May 11:S0896-6273(26)00315-6. PMID: 42119560
Cancer Lett

Vimentin binds to a novel tumor suppressor protein, GSPT1-238aa, encoded by circGSPT1 with a selective encoding priority to halt autophagy in gastric carcinoma. [Abstract]

2022 Oct 1:545:215826. PMID: 35839920
Cell Rep

TOR signaling regulates liquid phase separation of the SMN complex governing snRNP biogenesis. [Abstract]

2021 Jun 22;35(12):109277. PMID: 34161763
Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11;11:580407. PMID: 33343350
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
Mol Pain

Inhibition of mTOR/S6K1/Gli1 signaling alleviates morphine-induced thermal hyperalgesia and tolerance. [Abstract]

2025 Jan-Dec:21:17448069251376198. PMID: 40968661
ACS Chem Biol

Selective ATP-competitive inhibitors of TOR suppress rapamycin-insensitive function of TORC2 in Saccharomyces cerevisiae. [Abstract]

2012 Jun 15;7(6):982-7. PMID: 22496512
Hum Mol Genet

mTOR pathway repressing expression of FoxO3 is a potential mechanism involved in neonatal white matter dysplasia. [Abstract]

2022 Aug 17;31(15):2508-2520. PMID: 35220433
Vet Microbiol

The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]

2026 May:316:110992. PMID: 41865607
Exp Ther Med

Role of mTOR signaling in the regulation of high glucose-induced podocyte injury. [Abstract]

2019 Apr;17(4):2495-2502. PMID: 30906437
Biomed Pharmacother

Pharmacological effects of mTORC1/C2 inhibitor in a preclinical model of NASH progression. [Abstract]

2023 Nov:167:115447. PMID: 37683589
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 16.67 mg/mL (35.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1480 mL

10.7402 mL

21.4804 mL

5 mM

0.4296 mL

2.1480 mL

4.2961 mL

10 mM

0.2148 mL

1.0740 mL

2.1480 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.67 mg/mL (3.59 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.67 mg/mL (3.59 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.67 mg/mL (3.59 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

HEK-293 cells are freshly lysed in Hepes lysis buffer. Lysate (1-4 mg) is pre-cleared by incubating with 5-20 μL of Protein G-Sepharose conjugated to pre-immune IgG. The lysate extracts are then incubated with 5-20 μL of Protein G-Sepharose conjugated to 5-20 μg of either anti-Rictor or anti-Raptor antibody, or pre-immune IgG. All antibodies are covalently conjugated to Protein G-Sepharose. 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 washes with Hepes kinase buffer. For Raptor immunoprecipitates used for phosphorylating S6K1, for the initial two wash steps the buffer includes 0.5mol/LNaCl to ensure optimal kinase activity. GST-Akt1 is isolated from serum-deprived HEK-293 cells incubated with PI-103 (1 μM for 1 hour). GST-S6K1 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 10 mM MgCl₂ in the presence of various concentrations of KU-0063794 and GST-Akt1 (0.5 μg) or GST-S6K1 (0.5 μg). Reaction are carried out for 30 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-poresize Spin-X filter and samples are subjected to electrophoresis and immunoblot analysis with the indicated antibodies.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

Cells are treated with KU-0063794 for 24, 48, and 72 hours, and the medium is changed every 24 hours with freshly dissolved KU-0063794. For the measurement of cell growth, cells are washed once with PBS, and fixed in 4% (v/v) paraformaldehyde in PBS for 15 minutes. After washing once with water, the cells are stained with 0.1% Crystal Violet in 10% ethanol for 20 minutes and washed three times with water. Crystal Violet is extracted from cells with 0.5 mL of 10% (v/v) ethanoic (acetic) acid for 20 minutes. The eluate is then diluted 1:10 in water and absorbance at 590 nm is quantified. For the assessment of cell cycle distribution, cells are harvested by trypsinization, washed once in PBS, and re-suspended in ice-cold aq. 70% (v/v) ethanol. Cells are washed twice in PBS plus 1% (w/v) BSA and stained for 20 minutes in PBS plus 0.1% (v/v) Triton X-100 containing 50 g/mL propidium iodide and 50 g/mL RNase A. The DNA content of cells is determined using a FACSCalibur flow cytometer and CellQuest software. Red fluorescence (585 nm) is acquired on a linear scale, and pulse width analysis is used to exclude doublets. Cell-cycle distribution is determined using FlowJo software.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Garcia-Martinez et al. Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem.J. (2009)421 29. [Content Brief]

[2]. Collak FK, et al. Threonine-120 phosphorylation regulated by phosphoinositide-3-kinase/Akt and mammalian target of rapamycin pathway signaling limits the antitumor activity of mammalian sterile 20-like kinase 1.J Biol Chem. 2012 Jul 6;287(28):23698-709. E [Content Brief]

[3]. Haagensen EJ, et al. The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition. Br J Cancer. 2012 Apr 10;106(8):1386-94. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1480 mL	10.7402 mL	21.4804 mL	53.7011 mL
	5 mM	0.4296 mL	2.1480 mL	4.2961 mL	10.7402 mL
	10 mM	0.2148 mL	1.0740 mL	2.1480 mL	5.3701 mL
	15 mM	0.1432 mL	0.7160 mL	1.4320 mL	3.5801 mL
	20 mM	0.1074 mL	0.5370 mL	1.0740 mL	2.6851 mL
	25 mM	0.0859 mL	0.4296 mL	0.8592 mL	2.1480 mL
	30 mM	0.0716 mL	0.3580 mL	0.7160 mL	1.7900 mL

Keywords

KU-0063794

15 Cited Publications

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KU-0063794

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Lipid Metabolism Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) KU-0063794

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

KU-0063794 Related Classifications

HY-50710 Related Classifications