2. PROTAC Metabolic Enzyme/Protease
  3. PROTACs NAMPT
  4. Nampt degrader-2

Nampt degrader-2 是一种荧光 PROTAC，可有效降解 NAMPT，IC50 为 41.9 nM。Nampt degrader-2 与 NAMPT 和 VHL 结合形成三元复合物，随后通过泛素-蛋白酶体系统 (UPS) 诱导 NAMPT 降解。Nampt degrader-2 导致 NAD+ 显着减少并发挥有效的抗肿瘤活性。

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Nampt degrader-2 Chemical Structure

Nampt degrader-2 Chemical Structure

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Nampt degrader-2 相关抗体

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nampt degrader-2 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC50 of 41.9 nM. Nampt degrader-2 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). Nampt degrader-2 leads to significant reduction of NAD+ and exerts potent antitumor activities[1].

IC50 & Target[1]

VHL

 

NAMPT

41.9 nM (IC50)

体外研究
(In Vitro)

Nampt degrader-2 (Compound B4; 30 nM; 24 h) is able to degrade NAMPT with a DC50 value of 8.4 nM. Nampt degrader-2 enables the visualization of degradation in A2780 cells[1].
Nampt degrader-2 (Compound B4) shows the best antitumor activity in suppression of the proliferation in A2780 cells (IC50 = 12.1 nM)[1].

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

Nampt degrader-2 相关抗体:

Western Blot Analysis[1]

Cell Line: A2780 cells
Concentration: 30 nM
Incubation Time: 24 h
Result: Were able to degrade NAMPT in A2780 cells at the concentration of 30 nM.
体内研究
(In Vivo)

Nampt degrader-2 (Compound B4; 10-30 mg/kg; i.p; once a day; for 14 consecutive days) shows excellent antitumor effects in a dose-dependent manner. And Nampt degrader-2 significantly decreases the NAMPT levels in the tumors[1].

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

Animal Model: BALB/C nude female mice (4-5 weeks of age, 14-18 g) injected with A2780 cells[1]
Dosage: 10 mg/kg, 30 mg/kg
Administration: i.p; once a day; for 14 consecutive days
Result: Achieved excellent antitumor effects in a dose-dependent manner.
分子量

1052.33

Formula

C59H73N9O7S
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

Nampt degrader-2 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:

Nampt degrader-2Nampt degrader2Nampt degrader 2PROTACsNAMPTNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorPROTAC Nampt degraderVHLubiquitin-proteasome systemantitumor activitiesfluorescentInhibitorinhibitorinhibit

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目录号：
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