SETDB1-TTD-IN-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SETDB1-TTD-IN-1 

SETDB1-TTD-IN-1 是一种有效,选择性和内源性结合剂竞争性的 SETDB1-TTD 抑制剂,Kd 值为 88 nM。SETDB1-TTD-IN-1 可用于 SETDB1-TTD 关联的生物学功能和疾病的研究。

SETDB1-TTD-IN-1

SETDB1-TTD-IN-1 Chemical Structure

CAS No. : 2755823-12-0

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生物活性

SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD), with a Kd of 88 nM. SETDB1-TTD-IN-1 can be used for the research of biological functions and disease associations of SETDB1-TTD[1].

IC50 & Target

Kd: 88 nM (SETDB1-TTD)[1]

体外研究
(In Vitro)

SETDB1-TTD-IN-1 shows some activity for 53BP1 and JMJD2A, with Kds of 4.3 μM and 86 μM, respectively. SETDB1-TTD-IN-1 does not show activity against 14 of the 16 tested tudor domains (Kd>100 μM)[1].
SETDB1-TTD-IN-1 (2.5-40 μM) efficiently and dose-dependently stabilizes the SETDB1-TTD protein in HEK293T cells[1].
SETDB1-TTD-IN-1 (2.5-40 μM; 24 h) significantly affected the expression of 72 genes in human acute monocytic leukemia THP-1 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

469.58

Formula

C28H31N5O2

CAS 号

2755823-12-0

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.

参考文献
  • [1]. Guo Y, et, al. Structure-Guided Discovery of a Potent and Selective Cell-Active Inhibitor of SETDB1 Tudor Domain. Angew Chem Int Ed Engl. 2021 Apr 12;60(16):8760-8765.

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