GW280264X
Based on 9 publication(s) in Google Scholar
GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively. ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.30%
- CAS. Nr.: 866924-39-2
- Formel: C28H41N5O6S
- Molecular Weight:575.72
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) GW280264X
More- Cell. 2026 Jun 25;189(13):3883-3902.e23. [Abstract]
- Metabolism. 2025 May 15:156298. [Abstract]
- Cell Rep Med. 2025 Apr 28:102117. [Abstract]
- Br J Pharmacol. 2026 Apr 22. [Abstract]
- Int J Mol Sci. 2024 Apr 17;25(8):4404. [Abstract]
- Int J Mol Sci. 2024 Jan 23;25(3):1363. [Abstract]
- Mucosal Immunol. 2025 Sep 12:S1933-0219(25)00093-5. [Abstract]
- Mol Biol Cell. 2025 Apr 23:mbcE25020075. [Abstract]
- Research Square Preprint. 2023 Nov 23.
Customer Validation & Images
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Flow Cytometry
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WB
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ELISA
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Flow Cytometry
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WB
Biologische Aktivität
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ADAM17 8 nM (IC50) |
ADAM10 11.5 nM (IC50) |
The proliferation of GS-7 cells was significantly reduced upon treatment with GW280264X or ADAM10/17 co-knockdown[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Glioblastoma-initiating cells (GIC) GS-7 cells
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Concentration:0.1, 1, and 3 µM
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Incubation Time:48 hours
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Result:Proliferation of GIC is inhibited through inhibition of ADAM10 and ADAM17.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice[3]
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Dosage:100 µg/kg
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Administration:I.p. injected; every day for one week starting 4 h post-surgery
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Result:Showed significantly improved functional recovery compared to the control group.
Chemical Information
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CAS. Nr. 866924-39-2
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Appearance Solid
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Molecular Weight 575.72
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Formel C28H41N5O6S
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Color White to off-white
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SMILES
O=C(OCC1=CC=CC=C1)NCCCC[C@H](NC([C@H](CC(C)C)[C@@H](N(C=O)O)CCC)=O)C(NC2=NC=CS2)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (9)
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Journal Impact Factor
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Most Recent
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Cell
Cell-autonomous control of CAR signaling and receptor shedding via ADAM17-mediated proteolysis. [Abstract]2026 Jun 25;189(13):3883-3902.e23. PMID: 42143019 -
Metabolism
Chemical discovery of a novel MD2/ADAM17 dual-target inhibitor as a potential therapeutic candidate for saturated fatty acid-induced myocardial inflammatory injury. [Abstract]2025 May 15:156298. PMID: 40381836 -
Cell Rep Med
Characterization and comparative analysis of multifunctional natural killer cell engagers during antitumor responses. [Abstract]2025 Apr 28:102117. PMID: 40318632
GW280264X purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2025 Apr 28:102117. [Abstract]
Surface staining of TNF on Pan T or NK cells from 6 donors in the presence of DMSO or GW280264X (10 μM) post-4 h PMA/ionomycin stimulation.
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Br J Pharmacol
The metalloproteinase ADAM17 promotes acute lung inflammatory responses during pancreatitis. [Abstract]2026 Apr 22. PMID: 42021473 -
Int J Mol Sci
Regulation of Mertk Surface Expression via ADAM17 and γ-Secretase Proteolytic Processing. [Abstract]2024 Apr 17;25(8):4404. PMID: 38673989
GW280264X purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Apr 17;25(8):4404. [Abstract]
PMA-differentiated THP-1s (for 72 h) were treated for 4 h with either 3 µM of GW280264X (GW; ADAM17 inhibitor), 5 µM of DAPT (γ-secretase inhibitor), or 10 µM of MG132 (proteasomal inhibitor).
GW280264X purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Apr 17;25(8):4404. [Abstract]
THP-1s expressing the tagged construct were starved for 18 h in serum-free RPMI and treated for 3 h. Flow cytometry data shows positive GFPs without staining. As expected, CHX treatment after 3 h reduces the expression of the construct. Gas6-VK, used at a concentration > 10 nM, decreases the FLAG-PE signal more when compared to other treatments known to induce cleavage (PMA, LPS). GW280264X is used as a control for Mertk cleavage.
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Int J Mol Sci
2024 Jan 23;25(3):1363. PMID: 38338642
GW280264X purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Jan 23;25(3):1363. [Abstract]
ELISA of IL6R in the supernatant of A549 after 17 h incubation with either DMSO or GW280264X (1 μM).
GW280264X purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Jan 23;25(3):1363. [Abstract]
Western blots of STAT3 activation status (p-STAT3/STAT3) in A549 and HEP in the following conditions: without stimulus (BL), IL6 + PBS, or IL6 + sgp130Fc in the presence of either DMSO or GW280264X (1 μM).
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Mucosal Immunol
Neutrophil ADAM10 promotes migration and inflammation in ARDS by modulating adhesion and chemokine signaling. [Abstract]2025 Sep 12:S1933-0219(25)00093-5. PMID: 40947020 -
Mol Biol Cell
Deletion of the plexin-D1 ectodomain leads to anoikis by suppressing integrin inside-out signaling. [Abstract]2025 Apr 23:mbcE25020075. PMID: 40266804 -
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (173.70 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (604 KB)
- English - EN (604 KB)
- Français - FR (604 KB)
- Deutsch - DE (604 KB)
- Norwegian - NO (604 KB)
- Español - ES (604 KB)
- Swedish - SV (604 KB)
- Italian - IT (604 KB)
- Korean - KR (604 KB)
- Portuguese - PT (604 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Christian Hundhausen, et al. The disintegrin-like metalloproteinase ADAM10 is involved in constitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediated cell-cell adhesion. Blood. 2003 Aug 15;102(4):1186-95. [Content Brief]
[2]. Fabian Wolpert, et al. A disintegrin and metalloproteinases 10 and 17 modulate the immunogenicity of glioblastoma-initiating cells. Neuro Oncol. 2014 Mar;16(3):382-91. [Content Brief]
[3]. Daniela Sommer, et al. ADAM17-deficiency on microglia but not on macrophages promotes phagocytosis and functional recovery after spinal cord injury. Brain Behav Immun. 2019 Aug;80:129-145. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7370 mL | 8.6848 mL | 17.3696 mL | 43.4239 mL |
| 5 mM | 0.3474 mL | 1.7370 mL | 3.4739 mL | 8.6848 mL | |
| 10 mM | 0.1737 mL | 0.8685 mL | 1.7370 mL | 4.3424 mL | |
| 15 mM | 0.1158 mL | 0.5790 mL | 1.1580 mL | 2.8949 mL | |
| 20 mM | 0.0868 mL | 0.4342 mL | 0.8685 mL | 2.1712 mL | |
| 25 mM | 0.0695 mL | 0.3474 mL | 0.6948 mL | 1.7370 mL | |
| 30 mM | 0.0579 mL | 0.2895 mL | 0.5790 mL | 1.4475 mL | |
| 40 mM | 0.0434 mL | 0.2171 mL | 0.4342 mL | 1.0856 mL | |
| 50 mM | 0.0347 mL | 0.1737 mL | 0.3474 mL | 0.8685 mL | |
| 60 mM | 0.0289 mL | 0.1447 mL | 0.2895 mL | 0.7237 mL | |
| 80 mM | 0.0217 mL | 0.1086 mL | 0.2171 mL | 0.5428 mL | |
| 100 mM | 0.0174 mL | 0.0868 mL | 0.1737 mL | 0.4342 mL |
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