BromoTag® AGB1 is a highly selective and potent "Bump & Hole" TAG Degrader (DC50,6h < 15nM, T1/2 = 40 min). BromoTag AGB1 comprises a VHL E3 ligase ligand joined by a linker to a (+)-JQ1 derivative (the "bump" bearer) that selectively binds the Brd4BD2 L387A variant (the "hole"). In cell lines expressing a fusion of the target protein with the tag, Brd4BD2 L387A, BromoTag AGB1 drives formation of a ternary complex between VHL and the "BromoTagged" protein, leading to ubiquitination of the protein and its subsequent proteasomal degradation. BromoTag AGB1 is highly selective for Brd4BD2 L387A over wild-type, and is broadly selective across the proteome. BromoTag AGB1 exhibits no cytoxicity in several cancer relevant cell lines. BromoTag AGB1 is suitable for in vivo studies.
MedKoo Cat#: 466243
Name: BromoTag® AGB1
CAS#: 2776190-62-4
Chemical Formula: C51H63ClN8O9S2
Exact Mass: 1030.3848
Molecular Weight: 1031.68
Elemental Analysis: C, 59.37; H, 6.16; Cl, 3.44; N, 10.86; O, 13.96; S, 6.22
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 103.2 | 100.00 |
The following data is based on the product molecular weight 1,031.68 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
