2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. XMU-MP-10

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.

XMU-MP-10

XMU-MP-10 Chemical Structure

CAS No. : 2251132-02-0

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Based on 1 publication(s) in Google Scholar

XMU-MP-10 Related Antibodies

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Description

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[1].

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.

XMU-MP-10 Related Antibodies

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.
Molecular Weight

396.24

Formula

C18H14BrN5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5237 mL 12.6186 mL 25.2372 mL
5 mM 0.5047 mL 2.5237 mL 5.0474 mL
View the 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.

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Purity & Documentation
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
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XMU-MP-10 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XMU-MP-102251132-02-0E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseNEDD4TNBCCD8+ T cell,βTrCP/YAP/ECM axisInhibitorinhibitorinhibit

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