1. Epigenetics
  2. Histone Methyltransferase
  3. UNC8153

UNC8153 是一种强效且选择性的核受体结合 SET 结构域 2(NSD2)的降解剂,Kd 为 24 nM。UNC8153 可降低 NSD2 蛋白(U2OS 细胞中的 DC50 为 0.35 μM)和 H3K36me2 染色质标记的细胞水平。UNC8153 含有一个简单的弹头,可实现蛋白酶体依赖的 NSD2 降解。

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UNC8153 Chemical Structure

UNC8153 Chemical Structure

CAS No. : 2929304-60-7

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Other Forms of UNC8153:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2[1].

体外研究
(In Vitro)

UNC8153 (0-20 μM, 96 h) 在 KMS11 细胞中表现出抗粘附作用,并对 MM1S 细胞表现出轻微的细胞毒性[1]

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

Cell Proliferation Assay[1]

Cell Line: MM1S
Concentration: 0-50 μM
Incubation Time: 96 h
Result: Inhibited the cell proliferation.
分子量

583.68

Formula

C33H37N5O5

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
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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:
UNC8153
目录号:
HY-157251A
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