SIM1

Key Product Details

Product Description

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.

Licensing Information

Sold under licence from the University of Dundee

Product Specifications for SIM1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for SIM1

The following data is based on the product molecular weight 1618.82.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	1.24 mL	6.18 mL	12.35 mL
2.5 mM	0.25 mL	1.24 mL	2.47 mL
5 mM	0.12 mL	0.62 mL	1.24 mL
25 mM	0.02 mL	0.12 mL	0.25 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Imaide Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity Nat.Chem.Biol. 2021 PMID: 34675414

Product Documents for SIM1