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Tocris Bioscience™ SIM1
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Catalog No. 74325
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Quantity:
5 mg
This item is not returnable. View return policy
This item is not returnable. View return policy

Description

Potent and selective trivalent BET Bromodomain Degrader (PROTAC™)

SIM1 is a potent and selective trivalent PROTAC™ Degrader based on BET bromodomain inhibitors linked to a Von Hippel Lindau (VHL) ligand via branched linkers. SIM1 degrades all BET family proteins with a preference for BRD2 (DC50 values = 0.7 nM, 1.1 nM and 3.3 nM for BRD4, BRD2 and BRD3, respectively). SIM1 degrades BRD2 more significantly and rapidly than BRD3 and BRD4, and degrades BET proteins with a higher potency than a bivalent degrader. SIM1 also decreases protein levels for Myc and HMOX1 and induces apoptosis in prostate cancer cells.

Specifications

Chemical Name or Material N,N'-(11-((2-((-1-((2 S,4 R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)methyl)-11-methyl-3,6,9,13,16,19-hexaoxahenicosane-1,21-diyl)bis(2-(-4-(4-chlorophenyl)-2,3,9-tri
Quantity 5 mg
Target Active Degraders
Molecular Formula C79H98Cl2N14O13S3
Purity 0.98
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