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

XMU-MP-10 是一种 NEDD4 抑制剂 (KD 为43.92 nM)。XMU-MP-10 能选择性抑制 NEDD4 的自身泛素化，同时不影响其他泛素化活性。XMU-MP-10 能上调 β-TrCP 并导致 YAP 降解，且不改变 NEDD4 的蛋白表达水平。XMU-MP-10 通过增强 CD8+ T 细胞浸润，在体内表现出显著抑制三阴性乳腺癌肿瘤生长的功效。XMU-MP-10 通过 β-TrCP/YAP/ECM 轴增强抗肿瘤免疫反应。XMU-MP-10 可用于三阴性乳腺癌的相关研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

XMU-MP-10

XMU-MP-10 Chemical Structure

CAS No. : 2251132-02-0

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

XMU-MP-10 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

XMU-MP-10 与 NEDD4 的 HECT 结构域在 Y604、Y605 和 Y634 残基处发生相互作用[1]。
XMU-MP-10 (0.1-10000 μM) 特异性结合野生型 NEDD4，但不结合 Y604A、Y605A 或 Y634A 位点突变的 NEDD4 突变体[1]。
XMU-MP-10 (0.25-10 μM, 1-12 h) 以剂量依赖的方式显著抑制 NEDD4 的多聚泛素化，上调 β-TrCP 并导致 YAP 降解，此过程具有剂量和时间依赖性，且在 EMT6、4T1、MDA-MB-231 和 HCC38 细胞中不影响 NEDD4 蛋白的表达[1]。
XMU-MP-10 (2-10 μM, 4 h) 在 HEK-293T 细胞中选择性抑制 NEDD4 的自泛素化，而不影响其他被测 E3 连接酶的泛素化活性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

XMU-MP-10 相关抗体:

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.
体内研究
(In Vivo)

XMU-MP-10 (25 mg/kg，静脉注射，每日一次，持续 14 天) 在 4T1 细胞诱导的 BALB/c 小鼠中耐受性良好，但在 4T1 细胞诱导的 BALB/c-nu 小鼠中并未表现出良好耐受性[1]。
XMU-MP-10 (25 mg/kg，静脉注射，每日一次，持续 14 天) 在 EMT6 细胞诱导的 BALB/c 小鼠中，CD8+ T 细胞对其肿瘤抑制起关键作用，并影响 β-TrCP-YAP-ECM 轴[1]。
XMU-MP-10 (25 mg/kg，静脉注射，每日一次，持续 14 天) 在人源化免疫系统小鼠模型中，通过增加肿瘤内 CD8 阳性细胞毒性 T 细胞的浸润来增强抗肿瘤免疫反应[1]。

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.
分子量

396.24

Formula

C18H14BrN5O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

XMU-MP-10 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
XMU-MP-10
目录号：
HY-179570
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z