Butyrolactone 3
(Synonyms: 丁内酯 3; MB-3) 目录号 : GC10226Butyrolactone 3是组蛋白乙酰转移酶GCN5的小分子抑制剂（IC50 = 100μM）。
Cas No.:778649-18-6
Sample solution is provided at 25 µL, 10mM.
Butyrolactone 3 is a small molecule inhibitor of the histone acetyltransferase GCN5 (IC50 = 100μM) [1]. Butyrolactone 3 inhibits the catalytic activity of GCN5 to reduce histone acetylation levels and block downstream GCN5 signaling pathways, thereby disrupting tumor cell survival mechanisms [2-3]. Butyrolactone 3 is primarily used to treat lymphoma [4].
In C3H10T1/2 cells, Butyrolactone 3 (100μM; 4 weeks) inhibits the expression of Gcn5 after islet-1 transfection [5]. In H3K9ac cells, Butyrolactone 3 (0-200μM; 48h) inhibits GCN5 HAT activity and thus reduces the viability of burkitt lymphoma cells [6].
In ovarian cancer PDX mice model, Butyrolactone 3 (5mg/kg; ip; 30d) can increase the sensitivity of ovarian cancer cases to Cisplatin and even reverse their resistance [7]. In streptozotocin and a high fat diet rat model, Butyrolactone 3 (1mg/kg; nasal administrated; 8 weeks) attenuates increase in GCN5, H3K9 histone hyperacetylation on CDK5 promoter, and CDK5 upregulation [8].
References:
[1]. Mai A, Rotili D, Tarantino D, et al. Small-molecule inhibitors of histone acetyltransferase activity: identification and biological properties[J]. Journal of medicinal chemistry, 2006, 49(23): 6897-6907.
[2]. Haque M E, Jakaria M, Akther M, et al. The GCN5: its biological functions and therapeutic potentials[J]. Clinical Science, 2021, 135(1): 231-257.
[3]. Luan J, Chu Z, Chandra J, et al. Small molecular inhibitors targeting chromatin regulating proteins for cancer[J]. Current Protein and Peptide Science, 2016, 17(5): 455-462.
[4]. Gong Y, Fu W. Reversible role of MIR654/3P and MIR9/3P in pathogenesis of Epstein-Barr virus–negative, but not Epstein-Barr virus–positive, Burkitt lymphoma[J]. Journal of Leukocyte Biology, 2025, 117(3): qiae237.
[5]. Xu H, Zhou Q, Yi Q, et al. Islet-1 synergizes with Gcn5 to promote MSC differentiation into cardiomyocytes[J]. Scientific Reports, 2020, 10(1): 1817.
[6]. Farria A T, Mustachio L M, Akdemir Z H C, et al. GCN5 HAT inhibition reduces human Burkitt lymphoma cell survival through reduction of MYC target gene expression and impeding BCR signaling pathways[J]. Oncotarget, 2019, 10(56): 5847.
[7]. Sun C, Li X, Teng Q, et al. Targeting platinum-resistant ovarian cancer by disrupting histone and RAD51 lactylation[J]. Theranostics, 2025, 15(7): 3055.
[8]. Cai H B, Fan Z Z, Tian T, et al. Diabetes-induced H3K9 hyperacetylation promotes development of Alzheimer’s disease through CDK5[J]. Journal of Alzheimer’s Disease, 2020, 77(1): 75-84.
Butyrolactone 3是组蛋白乙酰转移酶GCN5的小分子抑制剂（IC50 = 100μM） [1]。Butyrolactone 3通过抑制GCN5的催化活性来降低组蛋白乙酰化水平，并阻断下游GCN5信号通路，从而破坏肿瘤细胞的存活机制 [2-3]。Butyrolactone 3主要用于治疗淋巴瘤 [4]。
在C3H10T1/2细胞中，Butyrolactone 3（100µM；4周）可抑制islet-1转染后Gcn5的表达 [5]。在H3K9ac细胞中，Butyrolactone 3（0-200μM；48h）可抑制GCN5 HAT活性，从而降低伯基特淋巴瘤细胞的存活率 [6]。
在卵巢癌PDX小鼠模型中，Butyrolactone 3（5mg/kg；ip；30d）可以增加卵巢癌病例对顺铂的敏感性，甚至逆转其耐药性 [7]。在链脲佐菌素和高脂饮食大鼠模型中，Butyrolactone 3（1mg/kg；鼻腔给药；8周）可以减弱GCN5、H3K9组蛋白在CDK5启动子上的高乙酰化以及CDK5的上调 [8]。
| Cell experiment [1]: | |
Cell lines | C3H10T1/2 cells |
Preparation Method | C3H10T1/2 cells were cultured in DMEM supplemented with 10% fetal bovine serum (FBS) and transfected with the lentiviral vectors islet-1 or GFP (MOI = 20) at 5µg/mL polybrene. After 24 hours of incubation at 37°C and 5% CO2, the medium was changed. The cells were divided into three groups: a blank control group (C3H10T1/2), a control group (lentiviral vector-transfected with GFP), and a group transfected with the lentiviral vector islet-1 (lentiviral vector-transfected with islet-1). The LV-islet-1 group was further divided into four subgroups based on the time of transfection: LV-islet-1-1w, LV-islet-1-2w, LV-islet-1-3w, and LV-islet-1-4w. 24h after LV-islet-1 or GFP transfection, Butyrolactone 3 (100µM) was added to the culture medium and treated for 4 weeks. The cells were defined as LV-islet-1 + Butyrolactone 3 group and control group + Butyrolactone 3 group. |
Reaction Conditions | 100µM; 4 weeks |
Applications | Butyrolactone 3 inhibits the expression of Gcn5 after islet-1 transfection. |
| Animal experiment [2]: | |
Animal models | Ovarian cancer PDX mice model |
Preparation Method | An ovarian cancer PDX model was established. Four-week-old female NCG (NOD/ShiLtJGpt-Prkdc em26Cd52 Il2rg em26Cd22 /Gpt) mice were purchased for use in PDX model development. Fresh tumor tissue was collected from individual patients, mechanically homogenized, and injected subcutaneously into the lower back or axilla of NCG mice. When the implanted tumors were stable for passage, equal lengths of tumor homogenate were implanted into new recipient NCG mice. Two weeks later, the mice were randomly divided into three groups: PBS + DMSO, Cisplatin (5mg/kg) + DMSO, and Cisplatin + Butyrolactone 3 (5mg/kg). |
Dosage form | 5mg/kg; ip; 30d |
Applications | Butyrolactone 3 can increase the sensitivity of certain ovarian cancer cases to Cisplatin and even reverse their resistance. |
References: | |
| 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. |
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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 | 542.9 μL | 2.7144 mL | 5.4289 mL |
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动物平均体重 | g | |
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动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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