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.
MedKoo Cat#: 465597
Name: SIM1
CAS#: unknown
Chemical Formula: C79H98Cl2N14O13S3
Exact Mass: 1616.5977
Molecular Weight: 1618.82
Elemental Analysis: C, 58.61; H, 6.10; Cl, 4.38; N, 12.11; O, 12.85; S, 5.94
| Solvent | mg/mL | mM | comments | |
|---|---|---|---|---|
| Solubility | ||||
| DMSO | 80.9 | 50.00 |
The following data is based on the product molecular weight 1,618.82 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
