| CAS NO: | 778649-18-6 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 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 SMILES | O=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation 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: |
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