GNE-495
Based on 11 publication(s) in Google Scholar
GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.49%
- CAS No.: 1449277-10-4
- Formule: C22H20FN5O2
- Masse moléculaire:405.42
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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Kinase Inhibitor Library
HY-L009
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MAPK Compound Library
HY-L010
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Anti-Cancer Compound Library
HY-L025
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Oxygen Sensing Compound Library
HY-L045
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Anti-Obesity Compound Library
HY-L087
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Targeted Diversity Library
HY-L099
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) GNE-495
More- Adv Sci (Weinh). 2024 Jun;11(24):e2306671. [Abstract]
- Cell Rep Med. 2026 May 19;7(5):102787. [Abstract]
- Cancer Lett. 2026 Feb 16:218336. [Abstract]
- Oncogene. 2023 May;42(18):1438-1452. [Abstract]
- J Biol Chem. 2024 Jun;300(6):107309. [Abstract]
- J Cell Sci. 2026 Feb 15;139(4):jcs264424. [Abstract]
- Life Sci Alliance. 2023 Jun 27;6(9):e202302196. [Abstract]
- J Toxicol Pathol. 2026.
- Technical University of Dresden. 2025.
- SSRN. 2025 Aug 6.
- bioRxiv. 2025 January 13.
Customer Validation & Images
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In Vivo Efficacy Study
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WB
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Cell Migration/Invasion Assay
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Cell Migration/Invasion Assay
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WB
Voir tous les produits spécifiques à Isoform MAP4K
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Activité biologique
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MAP4K4 3.7 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HUVEC | IC50 |
0.057 nM
Compound: 13, GNE-495
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Anti-angiogenesis activity in HUVEC assessed as inhibition of cell migration
Anti-angiogenesis activity in HUVEC assessed as inhibition of cell migration
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[PMID: 26288693] |
GNE-495 is a potent and selective MAP4K4 inhibitor with efficacy in retinal angiogenesis. GNE-495 shows the best balance of MAP4K4 inhibition, permeability, microsomal stability, and cellular potency[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1449277-10-4
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Appearance Solid
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Masse moléculaire 405.42
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Formule C22H20FN5O2
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Color Light yellow to yellow
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SMILES
O=C(C1=C2C=CC(C3=CC=CC(F)=C3)=NC2=C(N)N=C1)NC4CN(C(C5CC5)=O)C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (11)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Peptide Transporter 1-Mediated Dipeptide Transport Promotes Hepatocellular Carcinoma Metastasis by Activating MAP4K4/G3BP2 Signaling Axis. [Abstract]2024 Jun;11(24):e2306671. PMID: 38639383
GNE-495 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun;11(24):e2306671. [Abstract]
GNE-495 (0.2-10 µM; 24 h) dramatically diminished the expression of MAP4K4 in Huh7 and PLC/PRF/5 cells.
GNE-495 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun;11(24):e2306671. [Abstract]
GNE-495 (2 µM; 24 h). Representative images and quantification of the Huh7 and PLC/PRF/5 cells in the wound-healing migration assays.
GNE-495 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun;11(24):e2306671. [Abstract]
GNE-495 (2 µM; 24 h). Representative images and quantification of the migration and invasion of the Huh7 and PLC/PRF/5 cells in the Transwell assays.
GNE-495 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun;11(24):e2306671. [Abstract]
Protein expression of EMT‐associated proteins in HCC and PLC/PRF/5 cells treated with GNE-495 (2 µM; 24 h).
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Cell Rep Med
A human iPSC-derived sensory neuron platform for high-throughput discovery of neuroprotectants against chemotherapy-induced peripheral neuropathy. [Abstract]2026 May 19;7(5):102787. PMID: 42097147 -
Cancer Lett
MAP4K4 regulates the immune landscape of pancreatic tumor microenvironment and provides an opportunity for immunotherapy. [Abstract]2026 Feb 16:218336. PMID: 41707980
GNE-495 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2026 Feb 16:218336. [Abstract]
GNE-495 (3 mg/kg; i.p.; once daily for 3 weeks) reduced tumor burden in KPC (Pdx1-Cre x LSL-KRASG12D x LSL-TP53R172H) mice.
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Oncogene
MAP4K4 promotes ovarian cancer metastasis through diminishing ADAM10-dependent N-cadherin cleavage. [Abstract]2023 May;42(18):1438-1452. PMID: 36922678 -
J Biol Chem
Blockade of a novel MAP4K4-LATS2-SASH1-YAP1 cascade inhibits tumorigenesis and metastasis in luminal breast cancer. [Abstract]2024 Jun;300(6):107309. PMID: 38657867 -
J Cell Sci
A supracellular actin network transmits forces over long distances at the apical surface of squamous carcinoma cells. [Abstract]2026 Feb 15;139(4):jcs264424. PMID: 41568698 -
Life Sci Alliance
MAP4K4 regulates forces at cell-cell and cell-matrix adhesions to promote collective cell migration. [Abstract]2023 Jun 27;6(9):e202302196. PMID: 37369604 -
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Solvant et solubilité
DMSO : 2.17 mg/mL (5.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.22 mg/mL (0.54 mM); Clear solution
This protocol yields a clear solution of ≥ 0.22 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.2 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.22 mg/mL (0.54 mM); Clear solution
This protocol yields a clear solution of ≥ 0.22 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Rats, Mice and Pups [1]
For the brain cassette study, three male Sprague-Dawley (SD) rats are dosed with intravenous (IV) bolus of six test compounds (e.g., GNE-495; 0.5 mg/kg). For the mouse PK study, female CD-1 mice are administered IV bolus doses of GNE-495 (1 mg/kg). In addition, female CD-1 mice are administered GNE-495 (5 mg/kg) via oral (PO) gavage. A dosing volume of 2 mL/kg is used for the rat brain cassette PK and 5 mL/kg is used for all other dosing. Animals are not fasted prior to dose administration, and water and food are available ad libitum. Following administration of the compound of interest, three blood samples (~60 μL) are collected at each time point from individual mice up to either 9 or 24 hours post-dose using a serial sampling approach. Immediately upon collection, the blood is mixed with K2EDTA and stored on ice or in a chilled Kryorack prior to centrifugation to obtain plasma. Within 1 hr of collection, blood samples are centrifuged at approximately 1000-2000× g for 10-15 min at 4°C, and plasma is harvested. The plasma samples are stored at -70 to -80°C until analysis. For neonate PK, 3-day old CD1 pups are injected with 25 mg/kg and 50 mg/kg GNE-495 intraperitoneally, blood samples are collected at the time points indicated, retinas are collected one hour post-dose and snap frozen in liquid nitrogen and stored at -80°C until analysis. Plasma and retinal lysate concentrations are determined by LC/MS/MS.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4666 mL | 12.3329 mL | 24.6658 mL | 61.6644 mL |
| 5 mM | 0.4933 mL | 2.4666 mL | 4.9332 mL | 12.3329 mL |
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