2. PROTAC NF-κB Apoptosis
  3. PROTACs IKK Apoptosis
  4. PROTAC IKKβ degrader-1

PROTAC IKKβ degrader-1 是一种 IKKβ PROTAC 降解剂 (DC50 = 7.15 μM)。PROTAC IKKβ degrader-1 可诱导三阴性乳腺癌细胞凋亡 (Apoptosis)。PROTAC IKKβ degrader-1 可诱导三阴性乳腺癌细胞发生 G1 期细胞周期阻滞。PROTAC IKKβ degrader-1 对多种细胞具有抗增殖活性。PROTAC IKKβ degrader-1 可用于三阴性乳腺癌、结肠癌、肝癌、胰腺癌等癌症的相关研究。
(粉色: IKK 和 IKKβ 配体 (HY-N0141)；蓝色: Ligands for E3 Ligase 和 Cereblon 配体 (HY-14658)；黑色: 连接子)。

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PROTAC IKKβ degrader-1

PROTAC IKKβ degrader-1 Chemical Structure

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PROTAC IKKβ degrader-1 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 IKK 亚型特异性产品:

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IKK-α IKK-β IKK IKKε TBK1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC IKKβ degrader-1 is a IKKβ PROTAC degrader (DC50 = 7.15 μM). PROTAC IKKβ degrader-1 induces apoptosis (Apoptosis) in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 induces G1 phase cell cycle arrest in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 exhibits antiproliferative activity against a variety of cells. PROTAC IKKβ degrader-1 is applicable for research related to cancers such as triple-negative breast cancer, colon cancer, liver cancer, pancreatic cancer[1]. (Pink: IKK and IKKβ ligand (HY-N0141); Blue: Ligands for E3 Ligase and Cereblon ligand (HY-14658); Black: linker).

IC50 & Target[1]

Cereblon

 

IKK-β

7.15 μM (DC50)

体外研究
(In Vitro)

PROTAC IKKβ degrader-1 (Compound 8) 可强效抑制 MDA-MB-231、HCT116、HepG、Panc-1、MCF-7 细胞增殖，IC50 分别为 1.55、2.52、3.83、3.67、4.12 μM[1]。
PROTAC IKKβ degrader-1 (0-10 μM; 0-24 h) 可通过泛素-蛋白酶体系统在 MDA-MB-231 细胞中高效诱导 IKKβ 蛋白降解，其 DC50 为 7.15 μM，在 10 μM 处理 24 h 时降解率达 91.24%[1]。
PROTAC IKKβ degrader-1 (2-5 μM; 48 h) 可在 MDA-MB-231 细胞中强效诱导凋亡性细胞死亡，处理 48 h 后，2 μM 浓度下的总凋亡率为 46.43%，5 μM 浓度下为 61.37%[1]。
PROTAC IKKβ degrader-1 (2-5 μM) 可在 MDA-MB-231 细胞中诱导 G1 期细胞周期阻滞，在 2 μM 浓度下有 69.64% 的细胞处于 G1 期，5 μM 浓度下该比例为 71.15%[1]。

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

PROTAC IKKβ degrader-1 相关抗体:

Apoptosis Analysis[1]

Cell Line: MDA-MB-231
Concentration: 2 μM, 5 μM
Incubation Time: 48 h
Result: Induced dose-dependent increases in early and late apoptotic cell populations.
At 2 μM, total apoptotic rate was 46.43% (15.82% early + 30.61% late).
At 5 μM, total apoptotic rate was 61.37% (23.33% early + 38.04% late).
分子量

690.78

Formula

C37H46N4O9
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

PROTAC IKKβ degrader-1 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:

PROTAC IKKβ degrader-1PROTAC IKKβ degrader1PROTAC IKKβ degrader 1PROTACsIKKApoptosisIκB kinaseI kappa B kinase IKKβ PROTAC degraderMDA-MB-231 cellsHCT116 cellsHepG cellsPanc-1 cellsMCF-7 cellstriple-negative breast cancercolon cancerliver cancerpancreatic cancer
Inhibitorinhibitorinhibit

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