2. Immunology/Inflammation
  3. PD-1/PD-L1
  4. MS1-96

MS1-96 是一种具有口服活性的 PD-L1 (程序性死亡配体 1) 降解剂。MS1-96 能有效降低多种结直肠癌 (CRC) 细胞系中 PD-L1 蛋白的表达水平。MS1-96 可直接与 PD-L1 结合 (KD = 2.58 μM)，并增强 HIP1R 与 PD-L1 之间的相互作用，从而改变 PD-L1 在网格蛋白包被囊泡内的细胞内转运。MS1-96 可诱导 PD-L1 的异常 N-糖基化，导致蛋白不稳定并加速其溶酶体介导的降解。MS1-96 可用于结直肠癌的研究。

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

MS1-96

MS1-96 Chemical Structure

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

MS1-96 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

MS1-96 is an orally active PD-L1 (programmed death-ligand 1) degrader. MS1-96 effectively reduced PD-L1 protein levels across multiple colorectal cancer (CRC) cell lines. MS1-96 directly binds to PD-L1 (KD = 2.58 μM) and enhances the interaction between HIP1R and PD-L1, thereby altering the intracellular trafficking of PD-L1 within clathrin-coated vesicles. MS1-96 induces abnormal N-glycosylation of PD-L1, destabilizing the protein and hastening its lysosome-mediated degradation. MS1-96 can be used for the study of colorectal cancer[1].

IC50 & Target

PD-L1

2.58 μM (Kd)

体外研究
(In Vitro)

MS1-96 (10 μM，48 小时) 显著降低 RKO 细胞中 PD-L1 蛋白水平，但未降低 RKO 细胞中 PD-L1 mRNA 水平[1]。
MS1-96 (0-3 μM，0-48 小时) 以时间和剂量依赖的方式诱导 RKO 细胞中 PD-L1 降解[1]。
MS1-96 (1.5 μM，24 小时) 降低 RKO 和 LoVo 细胞表面 PD-L1 的水平[1]。
MS1-96 (1.5 μM，24 小时) 通过下调 RKO 和 LoVo 细胞中 PD-L1 的表达来破坏 PD-1/PD-L1 的相互作用[1]。
MS1-96 (1.5 μM，24 小时) 增强 T 细胞对 RKO 细胞的杀伤作用，并减少存活细胞的数量[1]。
MS1-96 (1.5 μM，24 小时) 可增加 RKO 细胞与活化 PBMC 共培养后 LDH 的释放，表明其细胞毒性增强[1]。
MS1-96 (1.5 μM，0-12 小时) 可促进 RKO 细胞中 PD-L1 的降解，而非抑制其翻译，从而降低 PD-L1 的表达水平[1]。
MS1-96 (1.5 μM) 通过溶酶体途径降解 RKO 细胞中的 PD-L1，该过程不依赖于蛋白酶体或自噬[1]。
MS1-96 可诱导 RKO 细胞中 PD-L1 在 N35、N192、N200 和 N219 位点发生异常的 N-糖基化[1]。

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

MS1-96 相关抗体:
体内研究
(In Vivo)

MS1-96 (0-400 mg/kg，口服，每日一次，连续 8-10 天) 通过下调 PD-L1 有效抑制 MC38 细胞异种移植小鼠的结直肠癌肿瘤生长，该活性严格依赖于 CD8+ T 细胞，且安全性良好[1]。
MS1-96 (0-400 mg/kg，口服，每日一次，连续 9 天) 未能抑制免疫缺陷型 MC38 细胞异种移植小鼠的肿瘤生长[1]。

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

Animal Model: C57BL/6 mice (female, 5 weeks old) were subcutaneously inoculated with 8 × 105 MC38 colorectal cancer cells[1].
Dosage: 0 mg/kg, 100 mg/kg, 200 mg/kg, 400 mg/kg
Administration: P.o., once daily for 8, 10 days
Result: The drug significantly inhibited the growth of MC38 tumors in a dose-dependent manner.
Tumor volume and weight were significantly reduced.
No significant change in mouse body weight indicated good drug tolerance.
Western blot analysis showed a significant decrease in PD-L1 protein levels in tumor tissues.
Depletion of CD8+ T cells alone or simultaneous depletion of CD4+ and CD8+ T cells had no anti-tumor effect.
Depletion of CD4+ T cells alone did not affect the anti-tumor effect.
Animal Model: Immunodeficient nude mice (female, 4 weeks old) were subcutaneously inoculated with 8 × 105 MC38 colorectal cancer cells[1].
Dosage: 0 mg/kg, 200 mg/kg, 400 mg/kg
Administration: P.o., once daily for 9 days
Result: Failed to inhibit the growth of MC38 tumors.
分子量

375.50

Formula

C25H29NO2
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

MS1-96 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:

MS1-96PD-1/PD-L1PD-1/Programmed death-ligand 1colorectal cancerantitumor immunityPD-L1lysosomal degradationHIP1RInhibitorinhibitorinhibit

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：
MS1-96
目录号：
HY-179558
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