13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
聯系人:高小姐
電話:021-59541103 021-60443211
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Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 1mg 5mg |
| CAS | 778649-18-6 |
| 別名 | N/A |
| 化學名 | rel-tetrahydro-4-methylene-5-oxo-2R-propyl-3S-furancarboxylic acid |
| 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 |
| 儲存條件 | Store at -20°C |
| 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 |
產品描述：
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.
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原創作者：上海莼試生物技術有限公司
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賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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