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Butyrolactone 3
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。
Butyrolactone 3图片
CAS NO:778649-18-6
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
Butyrolactone 3 (MB-3) 是组蛋白乙酰转移酶 Gcn5 (IC50=100 μM) 的特异性小分子抑制剂,与 Gcn5 酶的天然底物组蛋白 H3 具有相当的亲和力。
Cas No.778649-18-6
别名丁内酯 3; MB-3
化学名rel-tetrahydro-4-methylene-5-oxo-2R-propyl-3S-furancarboxylic acid
Canonical SMILESO=C1C([C@@H](C(O)=O)[C@H](CCC)O1)=C
分子式C9H12O4
分子量184.2
溶解度≤14mg/ml in ethanol;14mg/ml in DMSO;13mg/ml in dimethyl formamide
储存条件Store at -20°C,unstable in solution, ready to use.
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
文献引用
产品描述

IC50: 100 μM

Butyrolactone 3 is a histone acetyltransferase Gcn5 inhibitor.

The human histone acetyltransferase Gcn5 is identified as a prominent member of the GNAT family with high preference for histone H3 as a substrate.

In vitro: The analogs of butyrolactone 3 only showed a weak inhibition of CBP, while butyrolactone 3 led to an inhibition of Gcn5. It was important to see that in the presence of acetyl-CoA the Kd value for binding of histone H3 to Gcn5 or PCAF was around 100 mM. Moreover, the affinity of butyrolactone 3 to the Gcn5 enzyme was found to be comparable to that of the natural substrate H3 and could provide an good starting point for the study of SAR. In addition, a nonirreversible inhibition of Gcn5 could be determine, and thus a Michael addition of nucleophilic groups of the enzymeBs active side was unlikely. Therefore, the derivatization of gbutyrolactone 3 at position 2 might be a promising starting point for future SAR studies [1].

In vivo: So far, there is no animal in vivo data reported.

Clinical trial: Up to now, Butyrolactone 3 is still in the preclinical development stage.

Reference:
1. M. Biel, A. Kretsovali, E. Karatzali, et al. Design, synthesis, and biological evaluation of a small-molecule inhibitor of the histone acetyltransferase Gcn5. Angewandte Chemie International Edition 43, 3974-3976 (2004).