IBG1 | BRD4 degrader | Probechem Biochemicals

Chemical Structure : IBG1

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IBG1 (BRD2/BRD4 degrader)

货号: 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.

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生物&药学活性

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.

物理化学性质&存储条件

分子量	822.96
分子式	C44H38N8O5S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

1. Oliver Hsia, et al. Nature. 2024 Feb 21. doi: 10.1038/s41586-024-07089-6.

IBG1 (BRD2/BRD4 degrader)

生物&药学活性

物理化学性质&存储条件

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IBG1 (BRD2/BRD4 degrader)

生物&药学活性

物理化学性质&存储条件

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