1. MAPK/ERK Pathway Apoptosis
  2. JNK Apoptosis
  3. YL5084

YL5084 是一种共价 JNK 抑制剂,对 JNK2JNK3 的选择性高于 JNK1IC50 分别为 70 nM、84 nM 和 2173 nM。YL5084 表现出不依赖 JNK2 的抗增殖作用,并以不依赖 JNK2 的方式诱导细胞凋亡。

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YL5084 Chemical Structure

YL5084 Chemical Structure

CAS No. : 2440199-73-3

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查看 JNK 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YL5084, a covalent JNK inhibitor, exhibits selectivity for JNK2 and JNK3 over JNK1 with IC50s of 70 nM, 84 nM and 2173 nM, respectively. YL5084 exhibits JNK2-independent antiproliferative effects and induces apoptosis in a JNK2-independent manner[1].

IC50 & Target[1]

JNK2

70 nM (IC50)

JNK3

84 nM (IC50)

JNK1

2173 nM (IC50)

体外研究
(In Vitro)

YL5084 (0.001-100 μM; 72 小时) 在 MM.1S 细胞中表现出剂量依赖性抗增殖作用,GR50 值为 200-300 nM[1]
YL5084 (0.5, 2.5 μM; 24 小时) 诱导细胞凋亡[1]
YL5084 对 PIKFYVE (KdELECT 结合测定中的 KD=5000 nM) 表现出较弱的抑制作用[1]
YL5084 在人和小鼠微粒体中具有中等代谢稳定性,半衰期分别为 16 分钟和 11 分钟[1]

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

Cell Proliferation Assay[1]

Cell Line: Multiple myeloma (MM) cell lines
Concentration: 0.001-100 μM
Incubation Time: 72 h
Result: Displayed dose-dependent antiproliferative effects with GR50 values of 200-300 nM.

Apoptosis Analysis[1]

Cell Line: MM.1S cells
Concentration: 0.5, 2.5 μM
Incubation Time: 24 h
Result: Induced apoptosis as evidenced by an increased level of PARP cleavage, an increased level of cleavage of caspase 3, and an increased level of Annexin V/PI staining.
分子量

600.71

Formula

C35H36N8O2

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

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产品名称:
YL5084
目录号:
HY-149930
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