Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2719051-84-8 | [Synonyms]
| [Molecular Formula]
C79H98Cl2N14O13S3 | [Molecular Weight]
1618.81 |
Chemical Properties | Back Directory | [density ]
1.39±0.1 g/cm3(Predicted) | [solubility ]
Soluble to 50 mM in DMSO | [form ]
Solid | [pka]
13.52±0.46(Predicted) | [color ]
White to light yellow |
Hazard Information | Back Directory | [Biological Activity]
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. | [storage]
Store at -20°C |
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