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MI-192
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。
MI-192图片
CAS NO:1415340-63-4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
MI-192 是一种选择性 HDAC2 和 HDAC3 抑制剂,IC50 分别为 30 nM 和 16 nM。
Cas No.1415340-63-4
化学名N-(2-aminophenyl)-4-[(3,4-dihydro-4-methylene-1-oxo-2(1H)-isoquinolinyl)methyl]-benzamide
Canonical SMILESO=C1N(CC2=CC=C(C(NC3=CC=CC=C3N)=O)C=C2)CC(C4=CC=CC=C41)=C
分子式C24H21N3O2
分子量383.4
溶解度≤5mg/ml in DMSO;1mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MI-192 is a histone deacetylases (HDACs) inhibitor that preferentially inhibits HDAC2 and HDAC3 with IC50 values of 30 nM and 16 nM, respectively [1].

Histone acetylation is the most commonly employed mechanism utilized by transcription factors to activate gene expression. Conversely, histone deacetylation is the most common mechanism used to inactivate genes. Histone deacetylase inhibitors (HDACIs) are in advanced clinical development as cancer therapeutic agents [1].

MI-192 is a novel benzamide-based compound that had marked selectivity for the class I enzymes, HDAC2 and HDAC3. In HeLa cell extracts, MI-192 inhibited HDAC activity with IC50 value of 1.5 μM. MI-192 selectively inhibited recombinant HDAC2 and HDAC3 with IC50 values of 30 nM and 16 nM, respectively over HDAC1, 4, 6, 7, and 8 (IC50s = 4.8, 5, >10, 4.1, and >10 μM, respectively). MI-192 showed the greatest growth inhibitory effect against the leukemic cell lines with an effective dose of 0.1-0.4 μM. MI-192 was cytotoxic and promoted apoptosis and differentiation in leukaemic cell lines [1]. In the human prostate cancer cell line PC3, MI-192 significantly increased tubulin acetylation and ablated the dynamic behaviour of microtubules in live cells [2].

References:
[1].  Boissinot, M.,Inman, M.,Hempshall, A., et al. Induction of differentiation and apoptosis in leukaemic cell lines by the novel benzamide family histone deacetylase 2 and 3 inhibitor MI-192. Leukemia Research 36, 1304-1310 (2012).
[2].  Bacon T, Seiler C, Wolny M, et al. Histone deacetylase 3 indirectly modulates tubulin acetylation. Biochem J. 2015 Dec 15;472(3):367-77.