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PRMT5-IN-1 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PRMT5-IN-1 hydrochloride图片
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
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

PRMT5IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selectiveprotein arginine methyltransferase 5 (PRMT5)inhibitor with anIC50of 11 nM for PRMT5/MEP50.PRMT5IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions[1].

IC50& Target

IC50: 11 nM (PRMT5/MEP50)[1]

体外研究
(In Vitro)

PRMT5 IN-1 (compound 9; 0-500 nM) hydrochlorideinhibits the PRMT5/MEP50 complex [Kinact/KI=1.2×105M-1min-1] very rapidly with a Kinactof 0.068 min-1and a good binding affinity (KI=55 nM)[1].
PRMT5 IN-1 (0-1000 nM; 3 d; Granta-519 cells) hydrochloride inhibits the expression of cellular sDMA with an IC50value of 0.012 μM[1].
PRMT5 IN-1 (0-1 μM; 10 d; Granta-519 cells) hydrochloride inhibits cell proliferation in a dose-dependent manner with an IC50value of 0.06 μM[1].

Cell Viability Assay[1]

Cell Line:Granta-519 cells
Concentration:0, 0.0001524, 0.000457, 0.001372, 0.004115, 0.012346, 0.037037, 0.111111, 0.333333 and 1 μM
Incubation Time:10 days
Result:Inhibited cell proliferative, in which cells died on day 10 at high concentrations (0.3 and 1 μM).

Western Blot Analysis[1]

Cell Line:Granta-519 cells
Concentration:0, 0.05, 0.15, 0.46, 1.37, 4, 12, 37, 111, 333, 1000 nM
Incubation Time:3 days
Result:Inhibited cellular sDMA in Granta-519 cells in a dose-dependent manner.
分子量

455.29

性状

Solid

Formula

C19H20Cl2N4O5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)