2. PROTAC Epigenetics Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. PROTACs Aurora Kinase E1/E2/E3 Enzyme
  4. CCT400028

CCT400028 是一种靶向 Aurora A (AURKA) 激酶的 PROTACs 类降解剂。CCT400028 通过招募 cereblon (CRBN) E3 泛素连接酶，诱导靶点蛋白泛素化及蛋白酶体降解。CCT400028 靶向人源 Aurora 三种亚型 (A、B、C) 的 KD 值分别为 71 nM、2100 nM 和 >10000 nM，与人源 CRBN 的 IC50 为 6300 nM。CCT400028 可用于白血病、神经母细胞瘤、胶质瘤的相关研究。

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CCT400028

CCT400028 Chemical Structure

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CCT400028 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CCT400028 is a PROTACs-class degrader that targets the Aurora A (AURKA) kinase. CCT400028 induces ubiquitination and proteasomal degradation of target proteins by recruiting the cereblon (CRBN) E3 ubiquitin ligase. The KD values of CCT400028 against the three subtypes of human AURKA are 71 nM, 2100 nM and >10000 nM, respectively, and its IC50 against human CRBN is 6300 nM. CCT400028 is applicable to relevant research on leukemia, neuroblastoma and glioma[1].

IC50 & Target

Cereblon

 

Aurora A

71 nM (Kd)

Aurora B

2100 nM (Kd)

Aurora C

>10 μM (Kd)

体外研究
(In Vitro)

CCT400028 (0.001-10 μM；0-24 h) 无钩效应，可在 MV4-11 人源儿童白血病细胞中强效降解 Aurora A，6 h 时的 DC50 为 29 nM，达到 DCmax=85%；并在人儿科神经母细胞瘤 Kelly 细胞中诱导强效且持久 (24 h) 的 Aurora A 降解[1]。
CCT400028 (1 μM; 4 h) 在人儿科神经母细胞瘤 Kelly 细胞中的 Aurora A 降解活性，能够被蛋白酶体功能抑制剂、Cullin 环连接酶活性抑制剂、CRBN 结合抑制剂以及 Aurora A 结合抑制剂阻断 (抑制剂需提前预处理 2 h)[1]。
CCT400028 (0.01-10 μM；72 h) 可抑制人儿童白血病细胞 MV4-11 的活力，GI50 为 310 nM[1]。

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

CCT400028 相关抗体:

Western Blot Analysis[1]

Cell Line: Kelly human pediatric neuroblastoma cells
Concentration: 0.001-10 μM
Incubation Time: 4 h; 24 h
Result: Induced robust, sustained Aurora A depletion at both 4 h and 24 h. Reduced Aurora A levels to near-background at concentrations ≥0.1 μM by 4 h, and maintained this depletion at 24 h. Showed no hook effect across the tested concentration range.

Western Blot Analysis[1]

Cell Line: Kelly human pediatric neuroblastoma cells
Concentration: 1 μM (CCT400028; preceded by 2 h pre-incubation with 10 μM MG132 (HY-13259), 1 μM MLN4924 (HY-70062), 10 μM CC220 (HY-101291), 0.25-5 μM Alisertib (HY-10971))
Incubation Time: 4 h (CCT400028 co-treatment; 2 h pre-incubation with inhibitors)
Result: Induced robust, sustained Aurora A depletion at both 4 h and 24 h.
Showed no hook effect across the tested concentration range.
Induced Aurora A degradation that was completely blocked by pretreatment with the proteasome inhibitor MG132 (HY-13259) and the neddylation inhibitor MLN4924 (HY-70062).
Induced Aurora A degradation that was inhibited by pretreatment with the CRBN ligand CC220 (HY-101291) and the Aurora A inhibitor Alisertib (HY-10971).
分子量

878.39

Formula

C47H49ClFN7O7
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

CCT400028 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

CCT400028CCT 400028CCT-400028PROTACsAurora KinaseE1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseneuroblastomaE3 ubiquitin ligasecereblonproteasomal degradationCRBNAURKAleukemiagliomapediatric tumor cellsAurora AInhibitorinhibitorinhibit

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产品名称：
CCT400028
目录号：
HY-181311
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