PRMT5-IN-1 hydrochloride
目录号: PL15017 纯度: ≥99%
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中文名称
PRMT5-IN-1 hydrochloride
英文名称
PRMT5-IN-1 hydrochloride
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
PRMT5 IN-1 hydrochloride (compound 9) 是一种半缩醛胺,是一种有效的选择性蛋白精氨酸甲基转移酶5 (PRMT5) 抑制剂,抑制 PRMT5/MEP50 的 IC50 值为 11 nM。PRMT5 IN-1 hydrochloride 在生理条件下可以转化为醛并与 C449 反应形成共价加合物。
生物活性
PRMT5 IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC 50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.
性状
Solid
IC50 & Target[1][2]
IC50: 11 nM (PRMT5/MEP50)
体外研究(In Vitro)
PRMT5 IN-1 (compound 9; 0-500 nM) hydrochlorideinhibits the PRMT5/MEP50 complex [Kinact/KI=1.2×10 M min] very rapidly with a Kinact of 0.068 min and a good binding affinity (KI=55 nM).
PRMT5 IN-1 (0-1000 nM; 3 d; Granta-519 cells) hydrochloride inhibits the expression of cellular sDMA with an IC50 value of 0.012 μM.
PRMT5 IN-1 (0-1 μM; 10 d; Granta-519 cells) hydrochloride inhibits cell proliferation in a dose-dependent manner with an IC50 value of 0.06 μM. 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, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Lin H, et, al. Discovery of Potent and Selective Covalent Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors. ACS Med Chem Lett. 2019 May 22;10(7):1033-1038.
搜索质检报告(COA)

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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