| CAS NO: | 778649-18-6 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 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。 |
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).
m.cnreagent.com