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Barbadin
- Soluble in DMSO
- MF: C19H15N3OS
- MW: 333.41
Description
Barbadin is a selective β-arrestin/β2-adaptin interaction inhibitor with IC50 values of 19.1 μM and 15.6 μM for β-arrestin1 and β-arrestin2, respectively. Barbadin blocks agonist-promoted endocytosis of the β2-adrenergic receptor, V2 vasopressin receptor, and angiotensin II type 1 receptor by disrupting the interaction between β-arrestin and the AP2 adaptor complex.
β-Arrestins are key regulators of G protein-coupled receptor (GPCR) signaling, receptor desensitization, trafficking, and endocytosis. Barbadin selectively inhibits AP2-dependent receptor internalization without affecting β-arrestin-independent transferrin uptake or AP2-independent endothelin-A receptor internalization, making it a valuable tool for investigating GPCR trafficking and β-arrestin biology.
Key Features
- Selective β-arrestin/β2-adaptin interaction inhibitor
- IC50: 19.1 μM (β-arrestin1) and 15.6 μM (β-arrestin2)
- Blocks AP2-dependent GPCR endocytosis
- Inhibits β2-adrenergic, V2 vasopressin, and AT1 receptor internalization
- Selective tool for studying β-arrestin-mediated trafficking
Applications
- β-Arrestin signaling research
- GPCR trafficking and endocytosis studies
- AP2 adaptor complex investigations
- Receptor internalization research
- Cell signaling and chemical biology studies
More Information
| Parent CAS No. | 356568-70-2 |
|---|---|
| Chemical Name | 3-Amino-5-(4-benzylphenyl)thieno[2,3-d]pyrimidin-4(3H)-one |
| SMILES | C1(C2C3C(=O)N(N)C=NC=3SC=2)C=CC(CC2C=CC=CC=2)=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C19H15N3OS/c20-22-12-21-18-17(19(22)23)16(11-24-18)15-8-6-14(7-9-15)10-13-4-2-1-3-5-13/h1-9,11-12H,10,20H2 |
| InChiKey | OCBXPCSXEQQADU-UHFFFAOYSA-N |
| CID | 727640 |
| Short Description | β-Arrestin/β2-Adaptin inhibitor |
