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。
货号:ajcx38504
CAS:2755823-12-0
分子式:C28H31N5O2
分子量：469.58
溶解度:DMSO : 125 mg/mL (266.20 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存： 现货

Background:

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].

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].

[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.