Butyrolactone 3

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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。

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

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	184.2
Cas No.	778649-18-6
Formula	C₉H₁₂O₄
Solubility	≤14mg/ml in ethanol;14mg/ml in DMSO;13mg/ml in dimethyl formamide
Chemical Name	rel-tetrahydro-4-methylene-5-oxo-2R-propyl-3S-furancarboxylic acid
Canonical SMILES	O=C1C([C@@H](C(O)=O)[C@H](CCC)O1)=C
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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).