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MKC9989
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。
MKC9989图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍

MKC9989是一种HAA抑制剂,且能抑制IRE1α其IC50值在0.23μM至44μM的范围之间。

Cell experiment:

Human RPMI 8226 plasmacytoma cells are grown in monolayer culture using medium (DMEM) supplemented with 10% fetal calf serum (FCS) at 37℃ and 5% CO2. MKC9989 is prepared as 10 mM stocks in DMSO, stored at -20℃, and diluted in medium. Thapsigargin (Tg) is resuspended in DMSO and diluted in medium. Cells are grown to 50% confluency, treated with 1 μM Tg and/or 10 μM MKC9989 at the indicated time points. After incubation of cells for the indicated periods, cells are harvested[1].

文献引用
产品描述

MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.

At 10 μM concentration, MKC9989 completely inhibits both basal and thapsigargin induced splicing of XBP1 mRNA. These effects are observed even in cells pre-treated with thapsigargin, indicating that MKC9989 can fully reverse the onset of XPB1 splicing after the UPR is initiated. In parallel analysis, MKC9989, significantly stabilizes the RIDD target CD59 mRNA when co-administered with thapsigargin relative to thapsigargin treatment alone and modestly increases levels of CD59 mRNA in non-stressed cells, the latter likely reflects the inhibition of baseline RIDD activity. In contrast to effects on XBP1 splicing, MKC9989 moderately stabilizes CD59 levels when administered 2 hour post treatment with thapsigargin. Finally, the potency of MKC9989 against the splicing of XBP1 mRNA (EC50=0.33 μM) is comparable to its potency against RNA cleavage in vitro[1].

[1]. Sanches M, et al. Structure and mechanism of action of the hydroxy-aryl-aldehyde class of IRE1 endoribonuclease inhibitors. Nat Commun. 2014 Aug 28;5:4202.