1. Epigenetics Metabolic Enzyme/Protease
  2. Epigenetic Reader Domain E1/E2/E3 Enzyme
  3. LO-3-61

LO-3-61 是一种 JQ-1 (HY-13030) 类似物,带有截短的富马酰胺基团,属于具有 PROTAC (蛋白降解靶向嵌合体) 特性的 BRD4 降解剂。LO-3-61 通过 CUL4DCAF16 依赖性途径降解细胞中 BRD4 的长、短两种亚型。LO-3-61 在 MDA-MB-231 细胞中显示对 BRD3 和 BRD4 降解的选择性。

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LO-3-61

LO-3-61 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LO-3-61, a JQ-1 (HY-13030) analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells[1].

体外研究
(In Vitro)

LO-3-61 (0.1-1 μM, 24 h) 在 HEK293T 细胞 (WT, CUL4DCAF16 C173S, CUL4DCAF16 C178S) 中通过蛋白酶体介导 BRD4 的降解,这一效应在 DCAF16 敲除细胞中可被抑制[1]

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

Western Blot Analysis[1]

Cell Line: HEK293T cells (WT, CUL4DCAF16 C173S, CUL4DCAF16 C178S, DCAF16 KO)
Concentration: 0.1, 1 μM
Incubation Time: 24 h
Result: Degraded BRD4 when BTZ (1 μM) for 1 h prior to treatment in HEK293T cells (WT, CUL4DCAF16 C173S, CUL4DCAF16 C178S).
Did not affect the degradation of BRD4 in DCAF16 KO cells.
分子量

677.60

Formula

C32H30Cl2N8O3S

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
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  • 稀释计算器

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  • 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:
LO-3-61
目录号:
HY-175179
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