XMU-MP-10
Based on 1 Customer Validation
XMU-MP-10 is a selective NEDD4 inhibitor with a KD of 43.92 nM. XMU-MP-10 selectively inhibits NEDD4 auto-ubiquitination without affecting other ubiquitination activity, upregulates of β-TrCP and results YAP degradation without affecting NEDD4 protein expression. XMU-MP-10 exhibits significant in vivo efficacy in inhibiting TNBC tumor growth by enhancing CD8+ T cell infiltration. XMU-MP-10 enhances antitumor immune responses through the β-TrCP/YAP/ECM axis. XMU-MP-10 can be used for Triple-Negative Breast Cancer (TNBC) research.
For research use only. We do not sell to patients.
- Purity: 98.10%
- CAS No.: 2251132-02-0
- Formula: C18H14BrN5O
- Molecular Weight:396.24
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Oxygen Sensing Compound Library
HY-L045
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Ubiquitination Compound Library
HY-L050
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Liver Cancer Compound Library
HY-L101
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Inhibitors Library
HY-L158
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Mitophagy Compound Library
HY-L180
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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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Amino Acid Metabolism Compound Library
HY-L189
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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
XMU-MP-10 interacts with the HECT domain of NEDD4 at residues Y604, Y605, and Y634[1].
XMU-MP-10 (0.1-10000 μM) binds specifically to WT NEDD4, but not to NEDD4 mutants at Y604A, Y605A, or Y634A[1].
XMU-MP-10 (0.25-10 μM, 1-12 h) significantly inhibits the polyubiquitination of NEDD4 in a dose-dependent manner, upregulates of β-TrCP and results YAP degradation in a dose and time-dependent manner without affecting NEDD4 protein expression in EMT6, 4T1, MDA-MB-231 and HCC38 cells[1].
XMU-MP-10 (2-10 μM, 4 h) selectively inhibits NEDD4 auto-ubiquitination without affecting the ubiquitination activity of the other tested E3 ligases in HEK-293T cell[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EMT6, 4T1, MDA-MB-231 and HCC38
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Concentration:1, 2, 5 and 10 μM
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Incubation Time:1, 4, 8, 12 h
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Result:Induced YAP degradation in a dose-dependent manner by up regulating β-TrCP in murine TNBC tumor cells.
Induced YAP degradation in 4T1 cells in a time-dependent manner by up-regulating β-TrCP.
Induced YAP degradation in a dose-dependent manner by up regulating β-TrCP in human TNBC tumor cells.
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Cell Line:HEK-293T cell
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Concentration:2, 5 and 10 μM
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Incubation Time:4 h
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Result:Reduced NEDD4 protein expression, but E3 ligases from C2-WW-HECT subfamily, including NEDD4L, NEDL1, NEDL2, Smurf1, Smurf2, WWP1, WWP2, and ITCH.
XMU-MP-10 (25 mg/kg, i.v., daily for 14 days) has a crucial role for CD8+ T cells in tumor inhibition and influences the β-TrCP-YAP-ECM axis in EMT6 cells induced-BALB/c mice[1].
XMU-MP-10 (25 mg/kg, i.v., daily for 14 days) enhances antitumor immune response by increasing intratumoral infiltration of CD8 cytotoxic T cells in a humanized immune system mice mode[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4T1 cells (2.5×105 suspended in 100 μL PBS, i.v.) induced-female BALB/c mice (7 to 9 weeks) or female BALB/c-nu mice (7 to 9 weeks)[1]
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Dosage:25 mg/kg
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Administration:i.v., daily for 14 days
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Result:Showed the stable body weight; preserved blood parameters; liver, kidney, and heart functions; and unchanged H&E staining of major organs.
Significantly inhibited tumor growth and reduced tumor weight.
Observed no substantial therapeutic effect in immunodeficient hosts.
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Animal Model:EMT6 (2×105 suspended in 100 μL PBS, i.v.) induced-female BALB/c mice (7 to 9 weeks)[1]
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Dosage:25 mg/kg
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Administration:i.v., daily for 14 days
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Result:Increased intratumoral infiltration of CD8+ T cells in immunocompetent hosts.
Observed the decrease in YAP levels and upregulation of β-TrCP.
Decreased the ECM formation related proteins and Sirius red stained collagen deposition.
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Animal Model:Wild type MDA-MB-231 (3×106) cells induced huPBMC-NCG mice (8 weeks)
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Dosage:25 mg/kg
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Administration:i.v., daily for 14 days
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Result:Significantly reduced the TNBC tumor growth.
Significantly increased intratumoral CD8+ T cell infiltration and reduced collagen deposition.
Chemical Information
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CAS No. 2251132-02-0
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Appearance Solid
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Molecular Weight 396.24
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Formula C18H14BrN5O
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Color White to off-white
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SMILES
O=C(C1=CNC(C2=NNC3=NC=CC=C32)=C1)NCC4=CC=C(C=C4)Br
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 4.17 mg/mL (10.52 mM; ultrasonic and warming and heat to 60°C; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5237 mL | 12.6186 mL | 25.2372 mL | 63.0931 mL |
| 5 mM | 0.5047 mL | 2.5237 mL | 5.0474 mL | 12.6186 mL | |
| 10 mM | 0.2524 mL | 1.2619 mL | 2.5237 mL | 6.3093 mL |
XMU-MP-10 Related Classifications
HY-179570 Related Classifications
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