Chemical Structure : IBG1
CAS No.:
2684292-71-3
IBG1
(BRD2/BRD4 degrader)
Catalog No.: PC-21846Not For Human Use, Lab Use Only.
IBG1 is a PROTAC-like, specific degrader of BET bromodomain BRD2 and BRD4 with DC50 of 0.15 nM (BRD4), which comprises the BET family bromodomain inhibitor JQ1 tethered to E7820.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
IBG1 is a PROTAC-like, specific degrader of BET bromodomain BRD2 and BRD4 with DC50 of 0.15 nM (BRD4), which comprises the BET family bromodomain inhibitor JQ1 tethered to E7820, functions via CRL4-DCAF16.
IBG1 does not affect paralogue BRD3.
IBG1 functions via CRL-mediated ubiquitination and proteasomal degradation, and an unexpected DCAF15-independent mechanism.
IBG1-induced degradation of BRD2 and BRD4 is dependent on CRL4–DCAF16, IBG1 recruits DCAF16 to degrade BRD4.
IBG1 enhances the intrinsic interaction between the tandem bromodomain region of BRD4 and DCAF16.
IBG1 bivalently binds both BRD4 bromodomains.
Physicochemical Properties
|
M.Wt
|
822.96
|
|
Formula
|
C44H38N8O5S2
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
methyl (S)-2-(4-(4'-((4-(N-(3-cyano-4-methyl-1H-indol-7-yl)sulfamoyl)benzyl)carbamoyl)-[1,1'-biphenyl]-4-yl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate
|
References
1. Oliver Hsia, et al. Nature. 2024 Feb 21. doi: 10.1038/s41586-024-07089-6.
Contact Us
sales@probechem.com
