1. PROTAC
  2. PROTACs
  3. UNC8461

UNC8461 是一种 PROTAC,同时是招募 CRBN 的 PROTAC 分子 UNC8209 (HY-183098) 的一种阴性对照类似物。UNC8461 的 CRBN 配体上带有一个甲基取代基,可破坏与 CRBN 的结合。UNC8461 无法降低肾癌细胞中 TBK1、AAK1、GAK 和 AURKA 的蛋白水平。UNC8461 不能抑制肾癌细胞在 3D 软琼脂中的集落形成,仅对部分肾癌细胞的集落形成发挥轻微的部分抑制作用。
(粉色: TBK1 配体 (HY-183099);蓝色: Cereblon 配体 (HY-W586822);黑色: 连接子 (HY-23105))。

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UNC8461

UNC8461 Chemical Structure

1.  客户无需承担相应的运输费用。

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

UNC8461 is a PROTAC and is negative control CRBN-recruiting PROTAC analog of UNC8209 (HY-183098). UNC8461 features a methyl group substitution on its CRBN ligand to disrupt CRBN binding. UNC8461 fails to reduce TBK1, AAK1, GAK, and AURKA protein levels in renal cancer cells. UNC8461 does not suppress 3-D soft agar colony formation in renal cancer cells, and exerts modest, partial inhibition on colony formation in some renal cancer cells[1]. (Pink: TBK1 ligand (HY-183099); Blue: Cereblon ligand (HY-W586822); Black: linker (HY-23105)).

IC50 & Target[1]

Cereblon

 

体外研究
(In Vitro)

UNC8461 (1 μM; 4-24 h) 不会在 UMRC6、A498、UMRC2 或 769-P 肾透明细胞癌 (ccRCC) 细胞中诱导 TBK1、AAK1、GAK 或 AURKA 降解[1]
UNC8461 (1 μM; 4-6 weeks) 仅对 769-P、A498、UMRC6、UMRC2、786-O 和 Caki-1 肾透明细胞癌 (ccRCC) 细胞的集落形成表现出轻微的部分抑制作用[1]

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

Western Blot Analysis[1]

Cell Line: UMRC6, A498, UMRC2, 769-P
Concentration: 1 μM
Incubation Time: 4, 24 h
Result: Failed to reduce TBK1 protein levels in UMRC6, A498, UMRC2, and 769-P cells at both 4-hour and 24-hour timepoints.
Had no effect on reducing the abundance of AAK1, GAK, or AURKA proteins in UMRC6 and A498 cells after 24-hour incubation.
分子量

982.91

Formula

C46H60BrN7O12

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 *
= × ×

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:
UNC8461
目录号:
HY-183100
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