Barbadin
Based on 17 publication(s) in Google Scholar
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors. Barbadin can induce apoptosis.
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- Purity: 98.93%
- CAS No.: 356568-70-2
- 화학식: C19H15N3OS
- 분자량:333.41
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보관:Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Barbadin
More- Circulation. 2023 Jan 10;147(2):158-174. [Abstract]
- Nat Immunol. 2024 Nov;25(11):2057-2067. [Abstract]
- Nat Commun. 2026 Feb 26. [Abstract]
- Nat Commun. 2025 Dec 8;16(1):10938. [Abstract]
- Neuron. 2025 Nov 26:S0896-6273(25)00842-6. [Abstract]
- Cell Chem Biol. 2022 Jan 20;29(1):67-73.e3. [Abstract]
- Sci Signal. 2023 Apr 4;16(779):eabl4283. [Abstract]
- Biochem Pharmacol. 2026 Aug;250(Pt 2):118027. [Abstract]
- Cancer Gene Ther. 2025 Dec;32(12):1414-1427. [Abstract]
- Drug Des Devel Ther. 2024 Mar 11:18:781-799. [Abstract]
- Front Pharmacol. 2021 Apr 22:12:625289. [Abstract]
- Sci Rep. 2021 Feb 9;11(1):3426. [Abstract]
- iScience. 2024 May 22;27(6):110047. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2022 Jan;1869(1):119144. [Abstract]
- Eur J Immunol. 2024 Dec;54(12):e2451299. [Abstract]
- Microcirculation. 2026 May;33(4):e70063. [Abstract]
- bioRxiv. 2024 Jan 20.
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Bio/Physico-chemical Assay
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WB
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Cell Migration/Invasion Assay
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Bio/Physico-chemical Assay
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Flow Cytometry
All Arrestin Isoforms
More
Biological Activity
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Arrestin-3/β-Arrestin 2 |
Barbadin (4 h) treatment reduces cell viability and induces apoptosis[2].
Barbadin (2 h) treatment arrests breast cancer cells in G0/G1 phase[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA MB-231 cells
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Concentration:
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Incubation Time:4 hours
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Result:Exhibited morphological characteristics of apoptosis including shrinkage, rounding and detachment, the percent of cell viability was reduced to 69.1% and apoptosis was developed in 29.9% of cells starved with EBSS (Earle’s balanced salt solution).
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Cell Line:MDA MB-231 cells
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Concentration:
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Incubation Time:2 hours
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Result:Arrested 63.7% of cells in G0/G1 phase.
Chemical Information
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CAS No. 356568-70-2
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Appearance Solid
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분자량 333.41
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화학식 C19H15N3OS
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Color White to light yellow
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SMILES
O=C1C(C(C2=CC=C(CC3=CC=CC=C3)C=C2)=CS4)=C4N=CN1N
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Publications (17)
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Journal Impact Factor
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Most Recent
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Circulation
Cannabinoid Receptor 2-Centric Molecular Feedback Loop Drives Necroptosis in Diabetic Heart Injuries. [Abstract]2023 Jan 10;147(2):158-174. PMID: 36448459 -
Nat Immunol
2024 Nov;25(11):2057-2067. PMID: 39358444 -
Nat Commun
2026 Feb 26. PMID: 41748625 -
Nat Commun
Discovery of a β-arrestin-biased CCKBR agonist that blocks CCKBR-dependent long-term potentiation. [Abstract]2025 Dec 8;16(1):10938. PMID: 41360797 -
Neuron
2025 Nov 26:S0896-6273(25)00842-6. PMID: 41308645
Barbadin purchased from MedChemExpress. Usage Cited in: Neuron. 2025 Nov 26:S0896-6273(25)00842-6. [Abstract]
Barbadin (100 μM; 2 h) was used to inhibit β-arrestin signaling and could indeed eliminate the inhibitory effect of MF-8 on LTP.
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Cell Chem Biol
Activity-based, bioorthogonal imaging of phospholipase D reveals spatiotemporal dynamics of GPCR-Gq signaling. [Abstract]2022 Jan 20;29(1):67-73.e3. PMID: 34161786
Barbadin purchased from MedChemExpress. Usage Cited in: Cell Chem Biol. 2022 Jan 20;29(1):67-73.e3. [Abstract]
The β-arrestin inhibitor Barbadin (100 μM; 30 min) prolongs PLD activity downstream of PTHR1–Gq signaling in hPTHR1-293 cells.
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Sci Signal
Migration mediated by the oxysterol receptor GPR183 depends on arrestin coupling but not receptor internalization. [Abstract]2023 Apr 4;16(779):eabl4283. PMID: 37014928
Barbadin purchased from MedChemExpress. Usage Cited in: Sci Signal. 2023 Apr 4;16(779):eabl4283. [Abstract]
Migration of sDCs toward 100 nM 7α,25-OHC upon preincubation with DMSO (vehicle) or Barbadin (50-100 μM; 30 min). Barbadin significantly decreased the migration of sDCs toward 7α,25-OHC in a concentration-dependent manner.
Barbadin purchased from MedChemExpress. Usage Cited in: Sci Signal. 2023 Apr 4;16(779):eabl4283. [Abstract]
Analysis of 7α,25-OHC-induced signaling by GPR183 upon preincubation with either DMSO (vehicle) or Barbadin (50 μM; 1 h). Barbadin decreased ligand-induced β-arrestin1 and β-arrestin2 recruitment to GPR183 but not its G protein signaling.
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Biochem Pharmacol
Bosentan confers cardioprotection against cisplatin toxicity: Involvement of β-arrestin-linked ETA receptor signaling. [Abstract]2026 Aug;250(Pt 2):118027. PMID: 42069228 -
Cancer Gene Ther
GPR107: A key driver of breast cancer invasion and metastasis through collagen IV modulation. [Abstract]2025 Dec;32(12):1414-1427. PMID: 41073571 -
Drug Des Devel Ther
Qifu Yixin Formula Improves Heart Failure by Enhancing β-Arrestin2 Mediated the SUMOylation of SERCA2a. [Abstract]2024 Mar 11:18:781-799. PMID: 38500692
Barbadin purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2024 Mar 11:18:781-799. [Abstract]
Barbadin (50μM) inhibited β-arr2 expression compared with the blank control, together with the inhibition of SRECA2a and SUMO1 protein expression, and blocked the effect of QFYXF, which upregulated SERCA2a and SUMO1 expression in AngII-induced hypertrophic NRCMs.
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Front Pharmacol
Targeting PAR2 Overcomes Gefitinib Resistance in Non-Small-Cell Lung Cancer Cells Through Inhibition of EGFR Transactivation. [Abstract]2021 Apr 22:12:625289. PMID: 33967759 -
Sci Rep
2021 Feb 9;11(1):3426. PMID: 33564089 -
iScience
2024 May 22;27(6):110047. PMID: 38883814 -
Biochim Biophys Acta Mol Cell Res
PAR2 blockade reverses osimertinib resistance in non-small-cell lung cancer cells via attenuating ERK-mediated EMT and PD-L1 expression. [Abstract]2022 Jan;1869(1):119144. PMID: 34599981 -
Eur J Immunol
Chronic stimulation desensitizes β2-adrenergic receptor responses in natural killer cells. [Abstract]2024 Dec;54(12):e2451299. PMID: 39350450 -
Microcirculation
Adipose Triglyceride Lipase and Gpr40 Contribute to the Anti-Contractile Effect of Perivascular Adipose Tissue. [Abstract]2026 May;33(4):e70063. PMID: 42076883 -
용액&용해도
DMSO : 50 mg/mL (149.97 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (7.50 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.
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.
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.
순도&문서
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Beautrait A, et al. A new inhibitor of the β-arrestin/AP2 endocytic complex reveals interplay between GPCR internalization and signalling. Nat Commun. 2017 Apr 18;8:15054. doi: 10.1038/ncomms15054. [Content Brief]
[2]. Thoria Donia, et al. β-Arrestin inhibition induces autophagy, apoptosis, G0/G1 cell cycle arrest in agonist-activated V2R receptor in breast cancer cells. Med Oncol. 2021 Mar 15;38(4):38. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9993 mL | 14.9966 mL | 29.9931 mL | 74.9828 mL |
| 5 mM | 0.5999 mL | 2.9993 mL | 5.9986 mL | 14.9966 mL | |
| 10 mM | 0.2999 mL | 1.4997 mL | 2.9993 mL | 7.4983 mL | |
| 15 mM | 0.2000 mL | 0.9998 mL | 1.9995 mL | 4.9989 mL | |
| 20 mM | 0.1500 mL | 0.7498 mL | 1.4997 mL | 3.7491 mL | |
| 25 mM | 0.1200 mL | 0.5999 mL | 1.1997 mL | 2.9993 mL | |
| 30 mM | 0.1000 mL | 0.4999 mL | 0.9998 mL | 2.4994 mL | |
| 40 mM | 0.0750 mL | 0.3749 mL | 0.7498 mL | 1.8746 mL | |
| 50 mM | 0.0600 mL | 0.2999 mL | 0.5999 mL | 1.4997 mL | |
| 60 mM | 0.0500 mL | 0.2499 mL | 0.4999 mL | 1.2497 mL | |
| 80 mM | 0.0375 mL | 0.1875 mL | 0.3749 mL | 0.9373 mL | |
| 100 mM | 0.0300 mL | 0.1500 mL | 0.2999 mL | 0.7498 mL |