Butyrolactone I
Based on 1 Customer Validation
Butyrolactone I is an orally active and ATP-competitive inhibitor of CDK1. Butyrolactone I inhibits NF-κB, cdc2 kinase, Bax, ROS production, modulates the PERK/CHOP. Butyrolactone I mitigates heat-stress-induced Apoptosis. Butyrolactone I shows anti-inflammatory and intestinal protective activity. Butyrolactone I has antitumor effects against non-small cell lung, small cell lung, prostate cancer and leukemia. Butyrolactone I can be used in NASH research.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 87414-49-1
- Formula: C24H24O7
- Molecular Weight:424.44
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
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CDK1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BEAS-2B | IC50 |
>20 μM
Compound: 7
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Antiproliferative activity against human BEAS2B cells after 24 hrs by CCK8 assay
Antiproliferative activity against human BEAS2B cells after 24 hrs by CCK8 assay
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[PMID: 30392953] |
| HCC1806 | IC50 |
>20 μM
Compound: 7
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Antiproliferative activity against human HCC1806 cells after 24 hrs by CCK8 assay
Antiproliferative activity against human HCC1806 cells after 24 hrs by CCK8 assay
|
[PMID: 30392953] |
| HepG2 | IC50 |
>20 μM
Compound: 7
|
Antiproliferative activity against human HepG2 cells after 24 hrs by CCK8 assay
Antiproliferative activity against human HepG2 cells after 24 hrs by CCK8 assay
|
[PMID: 30392953] |
| HT-29 | IC50 |
>20 μM
Compound: 7
|
Antiproliferative activity against human HT-29 cells after 24 hrs by CCK8 assay
Antiproliferative activity against human HT-29 cells after 24 hrs by CCK8 assay
|
[PMID: 30392953] |
| PANC-1 | IC50 |
>20 μM
Compound: 7
|
Antiproliferative activity against human PANC1 cells after 24 hrs by CCK8 assay
Antiproliferative activity against human PANC1 cells after 24 hrs by CCK8 assay
|
[PMID: 30392953] |
| RBL-2H3 | IC50 |
13.5 μM
Compound: 1; BTL-1
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Antiallergic activity in rat RBL-2H3 cell model assessed as inhibition rate of IgE-mediated degranulation in by measuring beta-aminosidase
Antiallergic activity in rat RBL-2H3 cell model assessed as inhibition rate of IgE-mediated degranulation in by measuring beta-aminosidase
|
[PMID: 38640354] |
Butyrolactone I (20 μg/mL, concentration equivalent to IC50 value, 2 h) inhibits the cdc2 kinase activity in PC-14 cells[1].
Butyrolactone I (35-100 μM) inhibits cell proliferation and causes an incomplete cell cycle arrest in G2/M, resulting in occasional skipping of mitosis and subsequent cell cycle progression in human prostate cell lines (DU145, PC-3, LNCaP)[2].
Butyrolactone I (10-50 μM, 24 h) mitigates heat-stress-induced apoptosis in IPEC-J2 cells by modulating the ROS/PERK/CHOP signaling pathway[3].
Butyrolactone I (63-1,000 μM, 2 h) induces morphological and sporulation changes in A. terreus and enhances secondary metabolite production[4].
Butyrolactone I exhibits potent anti-cancer activity against HL-60 (human leukemia) cells and PC-3 cells with the IC50s value of 13.2 μM and 41.7 μM, respectively[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Butyrolactone-I (1-5 mg/kg, p.o., 14 days) alleviates intestinal barrier damage caused by DSS through regulating lactobacillus johnsonii and its metabolites in mice[6].
Butyrolactone I (10-40 mg/kg, p.o., from the 17th week to 24th week) attenuates inflammation in murine NASH by inhibiting the NF-κB signaling pathway[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (heat-stressed)[3]
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Dosage:1, 5 mg/kg
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Administration:Oral gavage (p.o.), 14 days
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Result:Downregulated HSP70 mRNA and mitigated weight loss.
Returned water intake and body temperature to normal levels.
Increased colon length.
Decreased Bax mRNA.
Inhibited the increases in the ROS and MDA levels.
Inhibited endoplasmic reticulum stress (ERS).
Inhibited p-PERK/PERK, p-eIF2α/eIF2α, ATF4, and CHOP.
Chemical Information
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CAS No. 87414-49-1
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Appearance Solid
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Molecular Weight 424.44
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Formula C24H24O7
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Color White to yellow
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SMILES
COC([C@]1(C(C2=CC=C(C=C2)O)=C(C(O1)=O)O)CC3=CC(C/C=C(C)\C)=C(C=C3)O)=O
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Synonyms
Olomoucin
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (235.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Nishio K, et al. Antitumor effects of butyrolactone I, a selective cdc2 kinase inhibitor, on human lung cancer cell lines. Anticancer Res. 1996 Nov-Dec;16(6B):3387-95. P [Content Brief]
[2]. Suzuki M, et al. Butyrolactone I induces cyclin B1 and causes G2/M arrest and skipping of mitosis in human prostate cell lines. Cancer Lett. 1999 Apr 26;138(1-2):121-30. [Content Brief]
[3]. Niu X, et al. Butyrolactone-I from Marine Fungal Metabolites Mitigates Heat-Stress-Induced Apoptosis in IPEC-J2 Cells and Mice Through the ROS/PERK/CHOP Signaling Pathway. Mar Drugs. 2024 Dec 17;22(12):564. [Content Brief]
[4]. Schimmel TG, et al. Effect of butyrolactone I on the producing fungus, Aspergillus terreus. Appl Environ Microbiol. 1998 Oct;64(10):3707-12. [Content Brief]
[5]. An X, et al. Isolation and identification of phase I metabolites of butyrolactone I in rats. Xenobiotica. 2017 Mar;47(3):236-244. [Content Brief]
[6]. Chen S, et al. Butyrolactone-I from marine fungi alleviates intestinal barrier damage caused by DSS through regulating lactobacillus johnsonii and its metabolites in the intestine of mice. J Nutr Biochem. 2025 Jan;135:109786. [Content Brief]
[7]. Tian-Qi C, et al. Butyrolactone I attenuates inflammation in murine NASH by inhibiting the NF-κB signaling pathway. Biochem Biophys Res Commun. 2022 Oct 20;626:167-174. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3560 mL | 11.7802 mL | 23.5605 mL | 58.9011 mL |
| 5 mM | 0.4712 mL | 2.3560 mL | 4.7121 mL | 11.7802 mL | |
| 10 mM | 0.2356 mL | 1.1780 mL | 2.3560 mL | 5.8901 mL | |
| 15 mM | 0.1571 mL | 0.7853 mL | 1.5707 mL | 3.9267 mL | |
| 20 mM | 0.1178 mL | 0.5890 mL | 1.1780 mL | 2.9451 mL | |
| 25 mM | 0.0942 mL | 0.4712 mL | 0.9424 mL | 2.3560 mL | |
| 30 mM | 0.0785 mL | 0.3927 mL | 0.7853 mL | 1.9634 mL | |
| 40 mM | 0.0589 mL | 0.2945 mL | 0.5890 mL | 1.4725 mL | |
| 50 mM | 0.0471 mL | 0.2356 mL | 0.4712 mL | 1.1780 mL | |
| 60 mM | 0.0393 mL | 0.1963 mL | 0.3927 mL | 0.9817 mL | |
| 80 mM | 0.0295 mL | 0.1473 mL | 0.2945 mL | 0.7363 mL | |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5890 mL |