[CAS NO. 356568-70-2] Barbadin
PRODUCTS SPECIFICATIONS [356568-70-2]
DESCRIPTION [356568-70-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 333.41 |
| Molecular Formula | C19H15N3OS |
| SMILES | O=C1C(C(C2=CC=C(CC3=CC=CC=C3)C=C2)=CS4)=C4N=CN1N |
5 Publications Citing Use of MCE
Summary
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC 50 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 [1] [2] .
IC50 & Target
IC50: 19.1 μM (β-arrestin1); 15.6 μM (β-arrestin2) [1]
In Vitro
Barbadin (4 h) treatment reduces cell viability and induces apoptosis
[2]
.
Barbadin (2 h) treatment arrests breast cancer cells in G0/G1 phase
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis [2]
| Cell Line: | MDA MB-231 cells |
| Concentration: | |
| Incubation Time: | 4 hours |
| 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). |
Cell Cycle Analysis [2]
| Cell Line: | MDA MB-231 cells |
| Concentration: | |
| Incubation Time: | 2 hours |
| Result: | Arrested 63.7% of cells in G0/G1 phase. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 149.97 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9993 mL | 14.9966 mL | 29.9931 mL |
| 5 mM | 0.5999 mL | 2.9993 mL | 5.9986 mL |
| 10 mM | 0.2999 mL | 1.4997 mL | 2.9993 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.50 mM); Clear solution
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.
- [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.
Synonyms