1. PROTAC MAPK/ERK Pathway
  2. PROTACs JNK
  3. PROTAC JNK1 degrader-1

PROTAC JNK1 degrader-1 是一种 JNK1 PROTAC 降解剂。PROTAC JNK1 degrader-1 可通过泛素-蛋白酶体系统和自噬-溶酶体通路诱导 JNK1 降解。PROTAC JNK1 degrader-1 可抑制 TGF-β1 诱导的上皮间质转化 (EMT)。PROTAC JNK1 degrader-1 可用于纤维化疾病、癌症转移的研究。
(粉色: Ligands for Target Protein for PROTAC 和 JNK 和 JNK1 配体 (HY-183006);蓝色: Drug Intermediate 配体 (HY-W037848);黑色: 连接子 (HY-B1008))。

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PROTAC JNK1 degrader-1

PROTAC JNK1 degrader-1 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC JNK1 degrader-1 is a JNK1 PROTAC degrader. PROTAC JNK1 degrader-1 induces JNK1 degradation via the ubiquitin-proteasome system and autophagy-lysosome pathway. PROTAC JNK1 degrader-1 inhibits TGF-β1-induced epithelial-mesenchymal transition (EMT). PROTAC JNK1 degrader-1 can be used for research on fibrotic diseases and cancer metastasis[1]. (Pink: Ligands for Target Protein for PROTAC and JNK and JNK1 ligand (HY-183006); Blue: Drug Intermediate ligand (HY-W037848); Black: linker (HY-B1008)).

IC50 & Target[1]

JNK1

 

体外研究
(In Vitro)

PROTAC JNK1 degrader-1 (HY12) (10-100 nM; 5 h) 可抑制纯化的 JNK1 激酶活性,在 100 nM 时抑制率为 86.01%,在 10 nM 时抑制率为 59.55%[1]
PROTAC JNK1 degrader-1 (1 μM; 24-48 h) 可在 BEAS-2B 细胞中通过泛素-蛋白酶体系统和自噬-溶酶体通路诱导强效的、剂量和时间依赖性 JNK1 降解,其 DC50 为 0.16 μM,在 1 μM 作用 48 h 时降解率达 70.40%[1]
PROTAC JNK1 degrader-1 (1 μM; 48 h) 可在 BEAS-2B 细胞中选择性降解 JNK1,对 JNK2、p38 或 ERK 的蛋白水平无显著影响[1]
PROTAC JNK1 degrader-1 (0.1-1 μM; 1 h pre-treatment, 48 h total) 可抑制 A549 细胞中 TGF-β1 诱导的上皮间质转化 (EMT),在 0.1 μM 浓度下逆转间质标志物的上调和上皮标志物的下调,并抑制 TGF-β1 诱导的 JNK1 表达[1]

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

Western Blot Analysis[1]

Cell Line: BEAS-2B human normal lung epithelial cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Degraded JNK1 protein.
Showed minimal impact on JNK2, p38, or ERK protein levels.
分子量

575.50

Formula

C29H31BrN6O2

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 *
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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.

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产品名称:
PROTAC JNK1 degrader-1
目录号:
HY-182796
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