Art. -Nr.: HY-179570

XMU-MP-10

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XMU-MP-10 is a selective NEDD4 inhibitor with a K_D 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.

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Reinheit: 98.10%
CAS. Nr.: 2251132-02-0
Formel: C₁₈H₁₄BrN₅O
Molecular Weight:396.24

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

XMU-MP-10 Chemical Structure

CAS. Nr.: 2251132-02-0

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

EMT6, 4T1, MDA-MB-231 and HCC38
Concentration:

1, 2, 5 and 10 μM
Incubation Time:

1, 4, 8, 12 h
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.

Western Blot Analysis^[1]

Cell Line:

HEK-293T cell
Concentration:

2, 5 and 10 μM
Incubation Time:

4 h
Result:

Reduced NEDD4 protein expression, but E3 ligases from C2-WW-HECT subfamily, including NEDD4L, NEDL1, NEDL2, Smurf1, Smurf2, WWP1, WWP2, and ITCH.

In Vivo

XMU-MP-10 (25 mg/kg, i.v., daily for 14 days) is well tolerated in 4T1 cells induced-BALB/c mice but not in 4T1 cells-induced BALB/c-nu mice^[1].
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.

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]
Dosage:

25 mg/kg
Administration:

i.v., daily for 14 days
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.

Animal Model:

EMT6 (2×10⁵ suspended in 100 μL PBS, i.v.) induced-female BALB/c mice (7 to 9 weeks)^[1]
Dosage:

25 mg/kg
Administration:

i.v., daily for 14 days
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.

Animal Model:

Wild type MDA-MB-231 (3×10⁶) cells induced huPBMC-NCG mice (8 weeks)
Dosage:

25 mg/kg
Administration:

i.v., daily for 14 days
Result:

Significantly reduced the TNBC tumor growth.
Significantly increased intratumoral CD8⁺ T cell infiltration and reduced collagen deposition.

Chemical Information

CAS. Nr. 2251132-02-0
Appearance Solid
Molecular Weight 396.24
Formel C₁₈H₁₄BrN₅O
Color White to off-white
SMILES

O=C(C1=CNC(C2=NNC3=NC=CC=C32)=C1)NCC4=CC=C(C=C4)Br
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

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

2.5237 mL

12.6186 mL

25.2372 mL

5 mM

0.5047 mL

2.5237 mL

5.0474 mL

10 mM

0.2524 mL

1.2619 mL

2.5237 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, 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.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
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)
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]. Su N, et al,. Inhibiting NEDD4 in triple-negative breast cancer cells reprograms tumor immune microenvironment via the β-TrCP/YAP/ECM axis. Cell Rep Med. 2025 Oct 21;6(10):102420. [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, 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

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XMU-MP-10

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Anti-Breast Cancer Compound Library

Anti-Liver Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

XMU-MP-10

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Anti-Breast Cancer Compound Library

Anti-Liver Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

XMU-MP-10 Related Classifications

HY-179570 Related Classifications