PRMT5-IN-1 hydrochloride

立即咨询

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。

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 [K_inact/K_I=1.2×10⁵M^-1min^-1] very rapidly with a K_inactof 0.068 min^-1and a good binding affinity (K_I=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)