Butyrolactone 3
(Synonyms: 丁内酯 3; MB-3) 目录号 : GC10226A HAT inhibitor
Cas No.:778649-18-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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).
| Cas No. | 778649-18-6 | SDF | |
| 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 | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.4289 mL | 27.1444 mL | 54.2888 mL |
| 5 mM | 1.0858 mL | 5.4289 mL | 10.8578 mL |
| 10 mM | 0.5429 mL | 2.7144 mL | 5.4289 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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