1. Epigenetics Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  2. Histone Methyltransferase PAK Bcl-2 Family
  3. WX2-43

WX2-43 是一种 PRMT5-KLF4 抑制剂 (采用 biotin-WX2-43 与 GST-PRMT5 检测的 Kd 为 11.0 nM)。WX2-43 结合于 PRMT5 上第 L400 至 M500 位氨基酸之间的区域。WX2-43 可有效阻断 KLF4 与 PRMT5 的相互作用,并抑制 KLF4 的甲基化。WX2-43 可降低 p21 水平并升高 Bax 水平。WX2-43 可抑制三阴性乳腺肿瘤的进展。WX2-43 可用于三阴性乳腺癌和结直肠癌的相关研究。

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

WX2-43

WX2-43 Chemical Structure

CAS No. : 723754-14-1

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WX2-43 is a PRMT5-KLF4 inhibitor (Kd of 11.0 nM: biotin-WX2-43 with GST-PRMT5). WX2-43 binds to the region between amino acids L400-M500 on PRMT5. WX2-43 efficiently intercepts the interaction between KLF4 and PRMT5, and blocks KLF4 methylation. WX2-43 decreases p21 levels and increases Bax levels. WX2-43 suppresses triple negative breast tumor progression. WX2-43 can be used in the research of triple-negative breast cancer and colorectal cancer[1][2].

IC50 & Target[1]

PRMT5

11.0 nM (Kd)

Bax

 

体外研究
(In Vitro)

WX2-43 (生物素化 WX2-43;0.1 nM-10 μM;孵育 2 小时) 与 PRMT5 结合,其 Kd 值为 11.0 nM[1]
WX2-43 (0.03-10 μM;作用 24 h) 以 KLF4 依赖的方式抑制经顺铂处理的 MEFs 细胞活力[1]
WX2-43 在三阴性乳腺癌 (TNBC) 细胞系中的活性更强 (EC50 0.44-0.96 μM),高于正常乳腺上皮细胞系 (EC50 3.62-23.34 μM)[1]
WX2-43 可在二维 (2D) AKPS 培养体系中诱导间充质样表型,改变克隆形态、大小及肌动蛋白细胞骨架,并降低 Ki-67+ 细胞的频率[2]

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

Cell Viability Assay[1]

Cell Line: KLF4+/+ MEFs, KLF4-/- MEFs
Concentration: 0, 0.03, 0.1, 0.3, 1, 3, 10 μM (WX2-43); 5 μM (cisplatin)
Incubation Time: 24 h
Result: Reduced viability in KLF4+/+ MEFs in a dose-dependent manner; showed no effect on viability in KLF4-/- MEFs.

Western Blot Analysis[1]

Cell Line: MDA-MB-231
Concentration: 0, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Decreased KLF4 protein levels and p21 levels and increased Bax levels in a dose-dependent manner.
体内研究
(In Vivo)

WX2-43 (40-80 mg/kg;腹腔注射;每周 2 次;持续 4 周) 可抑制裸鼠体内三阴性乳腺癌的肿瘤进展[1]

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

Animal Model: Crl: Nu-Foxn1(nu) (female, 8 weeks old)[1]
Dosage: 40 mg/kg; 80 mg/kg
Administration: i.p.; twice weekly; 4 weeks
Result: Reduced tumor size and weight by approximately 40% at 40 mg/kg compared to vehicle; Reduced tumor size and weight by approximately 60% at 80 mg/kg compared to vehicle; Confirmed reduced KLF4 protein levels in treated groups via western blotting.
分子量

288.82

Formula

C17H21ClN2

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
  • 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.

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:
WX2-43
目录号:
HY-W072962
需求量: