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| 100mg |
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Purity: ≥98%
Brefeldin A (also known as BFA), a fungal metabolite, is a potent macrocyclic lactone antibiotic and ATPase inhibitor for intracellular vesicle formation and protein transport (protein trafficking between the endoplasmic reticulum (ER) and the Golgi apparatus) with IC50 of 0.2 μM in HCT 116 cells. It has antitumor, antifungal, and antiviral effects. It induces cancer cell differentiation and apoptosis. Treatment with BFA could attenuate stimulus-dependent hyperalgesia phenomenon via inhibiting vesicular exocytosis which process is important for ATP release. BFA induced cells apoprosis (colorectal cancer cell line HCT116 ) by inhibiting ATP which functioned in the process of cellular vesicle trafficking.
| ln Vitro |
After 15 or 40 hours of treatment with brefeldin A (BFA), the endoplasmic reticulum (ER) swells significantly and moves to the periphery of normal kidney (NRK) cells. Actin and MT cytoskeleton are significantly disrupted by prolonged Brefeldin A therapy [1]. Brefeldin A and ADPR conjugate mediates the ADP-ribosylation of BARS. When created with cells obtained from CD38+ HeLa cells treated with BFA, bars demonstrate BAC binding [3]. Brefeldin A reduces MDA-MB-231 colony formation in 3D and 2D cultures, promotes identity-independent cell death in MDA-MB-231 breast cancer cells, and blocks MDA-MB migration and MMP 9 (matrix metal Peptidase 9) activity-231[2].
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| ln Vivo |
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| References |
[1]. Alvarez C, et al. Brefeldin A (BFA) disrupts the organization of the microtubule and the actin cytoskeletons. Eur J Cell Biol. 1999 Jan;78(1):1-14.
[2]. Tseng CN, et al. Brefeldin A reduces anchorage-independent survival, cancer stem cell potential and migration of MDA-MB-231 human breast cancer cells. Molecules. 2014 Oct 29;19(11):17464-77. [3]. Wang J, et al. Erythroleukemia cells acquire an alternative mitophagy capability. Sci Rep. 2016 Apr 19;6:24641. [4]. Colanzi A, et al. Molecular mechanism and functional role of brefeldin A-mediated ADP-ribosylation of CtBP1/BARS. Proc Natl Acad Sci U S A. 2013 Jun 11;110(24):9794-9. [5]. Yu C, et al. Small molecules enhance CRISPR genome editing in pluripotent stem cells. Cell Stem Cell. 2015 Feb 5;16(2):142-7. [6]. Nozawa N, et al. Subcellular localization of herpes simplex virus type 1 UL51 protein and role of palmitoylation in Golgi apparatus targeting. J Virol. 2003 Mar;77(5):3204-16. [7]. Jensen HL, Rygaard J, Norrild B. A time-related study of Brefeldin A effects in HSV-1 infected cultured human fibroblasts. APMIS. 1995;103(7-8):530-539. doi:10.1111/j.1699-0463.1995.tb01402.x |
| Molecular Formula |
C16H24O4
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| Molecular Weight |
280.36
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| CAS # |
20350-15-6
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| Related CAS # |
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| SMILES |
O([H])[C@]1([H])C([H])([H])[C@]2([H])C([H])=C([H])C([H])([H])C([H])([H])C([H])([H])[C@@]([H])(C([H])([H])[H])OC(C([H])=C([H])C([H])([C@@]2([H])C1([H])[H])O[H])=O |c:10,t:31|
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| InChi Key |
KQNZDYYTLMIZCT-KQPMLPITSA-N
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| InChi Code |
InChI=1S/C16H24O4/c1-11-5-3-2-4-6-12-9-13(17)10-14(12)15(18)7-8-16(19)20-11/h4,6-8,11-15,17-18H,2-3,5,9-10H2,1H3/b6-4+,8-7+/t11-,12+,13-,14+,15+/m0/s1
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| Chemical Name |
(1S,2E,7S,10E,12R,13R,15S)-12,15-Dihydroxy-7-methyl-8-oxabicyclo[11.3.0]hexadeca-2,10-dien-9-one
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.92 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (8.92 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (8.92 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: ≥ 2.5 mg/mL (8.92 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5668 mL | 17.8342 mL | 35.6684 mL | |
| 5 mM | 0.7134 mL | 3.5668 mL | 7.1337 mL | |
| 10 mM | 0.3567 mL | 1.7834 mL | 3.5668 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05969353 | Recruiting | Other: accupunture | Assessing the Effectiveness of BFA as a Non-pharmacologic Pain Management Intervention: A Randomised Sham Controlled Study |
Bnai Zion Medical Center | July 23, 2023 | Not Applicable |
| NCT04094246 | Recruiting | Procedure: Battlefield Acupuncture | Shoulder Injuries Pain,Postoperative |
Keller Army Community Hospital | September 25, 2019 | Not Applicable |
| NCT06333938 | Not yet recruiting NEW |
Device: Bridge Device: BFA |
Anesthesia Surgery |
Durham VA Medical Center | June 2024 | Phase 4 |
| NCT06128772 | Not yet recruiting | Other: Battlefield Acupuncture | Chronic Pain Substance Use Disorders |
Edith Nourse Rogers Memorial Veterans Hospital |
November 30, 2023 | Not Applicable |
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Inhibition of intracellular protein trafficking by Brefeldin A |
Brefeldin A inhibits STING-induced IRF activity in THP1-Dual™ cells |
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