2. PROTAC Metabolic Enzyme/Protease
  3. PROTACs NAMPT
  4. PROTAC NAMPT Degrader-28

PROTAC NAMPT Degrader-28 是一种 NAMPT PROTAC 降解剂，在 MCF7 和 4T1cl5 细胞中的 DC50 值分别为 45 和 55 nM。PROTAC NAMPT Degrader-28 保留烟酰胺磷酸核糖转移酶抑制活性，且不会诱导该酶降解。PROTAC NAMPT Degrader-28 可用于乳腺癌相关研究。
(粉色: NAMPT 配体 (HY-181881)；蓝色: VHL 配体 (HY-112078)；黑色: 连接子 (HY-W018678))。

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PROTAC NAMPT Degrader-28

PROTAC NAMPT Degrader-28 Chemical Structure

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PROTAC NAMPT Degrader-28 相关抗体

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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

PROTAC NAMPT Degrader-28 is a NAMPT PROTAC degrader with DC50 values of 45 nM and 55 nM in MCF7 and 4T1cl5 cells, respectively. PROTAC NAMPT Degrader-28 retains nicotinamide phosphoribosyltransferase inhibitory activity and does not induce degradation of this enzyme. PROTAC NAMPT Degrader-28 can be used in breast cancer-related research[1]. (Pink: NAMPT ligand (HY-181881); Blue: VHL ligand (HY-112078); Black: linker (HY-W018678)).

IC50 & Target[1]

VHL

 

体外研究
(In Vitro)

PROTAC NAMPT Degrader-28 (Compound U42) (5 nM-4 μM; 1 h) 可抑制重组小鼠 NAMPT 的催化活性，其 IC50 为 417.5 nM[1]。
PROTAC NAMPT Degrader-28 (10 nM-1 μM; 72 h) 可强效降低 MCF7 和 4T1cl5 乳腺癌细胞的活力，其 IC50 值分别为 110 nM 和 157 nM[1]。
PROTAC NAMPT Degrader-28 (300 nM; 24 h, 48 h) 可在处理 24 h 和 48 h 后显著降低 MCF7 和 4T1cl5 乳腺癌细胞内的 NAD+水平[1]。
PROTAC NAMPT Degrader-28 (1-3 μM; 8 days) 可抑制 3D 乳腺癌细胞培养物中的乳腺球形成并诱导 NAMPT 降解，同时在处理 8 天后降低细胞外 NAMPT 水平[1]。
PROTAC NAMPT Degrader-28 (10 μM; 5 h) 可在 MCF7 和 4T1cl5 乳腺癌细胞中稳定 NAMPT 和 VHL 蛋白以抵抗热变性，证实 PROTAC NAMPT Degrader-28、NAMPT 与 VHL 之间形成了三元复合物[1]。

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

PROTAC NAMPT Degrader-28 相关抗体:

Western Blot Analysis[1]

Cell Line: MCF7 human breast cancer cells, 4T1cl5 murine triple-negative breast cancer cells
Concentration: 0.03, 0.1, 0.3, 0.6 and 1 μM; 300 nM (with bortezomib pre-treatment for 30 min; with inhibitor 7 or VHL-Ac pre-treatment for 1 h)
Incubation Time: 18 h
Result: Induced NAMPT degradation in a dose-dependent manner, with DC50 values of 45 nM in MCF7 cells and 55 nM in 4T1cl5 cells.
Blocked NAMPT degradation when co-treated with bortezomib.
Abolished NAMPT degradation when pre-treated with inhibitor 7 or VHL-Ac in both cell lines.
Did not affect NAPRT protein levels in either cell line.

Cell Viability Assay[1]

Cell Line: MCF7 human breast cancer cells, 4T1cl5 murine triple-negative breast cancer cells
Concentration: 10 nM, 30, 100, 300, 600 and 1 μM
Incubation Time: 72 h
Result: Reduced cell viability with IC50 values of 110 nM in MCF7 cells and 157 nM in 4T1cl5 cells.

Western Blot Analysis[1]

Cell Line: MCF7 human breast cancer cells, 4T1cl5 murine triple-negative breast cancer cells
Concentration: 0.1. 0.3, 1 and 3 μM
Incubation Time: 18 h (complete medium) followed by 18 h (serum-free medium)
Result: Induced dose-dependent degradation of eNAMPT in both cell lines, with significant reductions observed at 0.1, 0.3, and 1 μM.
分子量

1024.32

Formula

C58H73N9O6S
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 NAMPT Degrader-28 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)

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The dilution calculator equation

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

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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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:

PROTAC NAMPT Degrader-28PROTAC NAMPT Degrader28PROTAC NAMPT Degrader 28PROTACsNAMPTNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factornicotinamide phosphoribosyltransferasecereblonNAPRTMCF7 cellsVHLNAD+proteasomerecombinant murine NAMPTbreast cancer4T1cl5 cellsInhibitorinhibitorinhibit

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