SETDB1-TTD-IN-1
目录号: PL15046 纯度: ≥99%
CAS No. :2755823-12-0
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中文名称
SETDB1-TTD-IN-1
英文名称
SETDB1-TTD-IN-1
英文别名
4H-Pyrrolo[3,2-d]pyrimidin-4-one, 3,5-dihydro-2-[[(3R,5R)-1-methyl-5-[4-(phenylmethoxy)phenyl]-3-piperidinyl]amino]-3-(2-propen-1-yl)-;SETDB1-TTD-IN-1
Cas No.
2755823-12-0
分子式
C28H31N5O2
分子量
469.58
包装储存
4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
产品详情
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。
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 K d of 88 nM. SETDB1-TTD-IN-1 can be used for the research of biological functions and disease associations of SETDB1-TTD.
性状
Solid
IC50 & Target[1][2]
Kd: 88 nM (SETDB1-TTD)
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).
SETDB1-TTD-IN-1 (2.5-40 μM) efficiently and dose-dependently stabilizes the SETDB1-TTD protein in HEK293T cells.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
溶解度数据
In Vitro: DMSO : 125 mg/mL (266.20 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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