| MDL | - |
|---|---|
| Molecular Weight | 852.94 |
| Molecular Formula | C40H40N10O8S2 |
| SMILES | O=C(N(C(CCC1=O)C(N1)=O)C2=O)C(C2=CC=C3)=C3OCC(NCCCCN4C=C(COC5=CC(CC6=CN=C(NC(CSC7=NC(C)=CC(C)=N7)=O)S6)=CC=C5)N=N4)=O |
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC , acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC 50 of 0.25 μM for Sirt2 , with no effect on Sirt1/Sirt3 (IC 50 s>100 μM) [1] .
|
SIRT2 0.25 μM (IC 50 ) |
PROTAC Sirt2 Degrader-1 (Compound 12; 10 µM, 1-6 hours) induces Sirt2 degradation in HeLa cells [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | HeLa cells |
| Concentration: | 10 µM |
| Incubation Time: | 1-6 hours |
| Result: | Caused Sirt2 degradation, but showed no effect on Sirt1 levels. |
Solid
Room temperature in continental US; may vary elsewhere.
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
DMSO : ≥ 100 mg/mL ( 117.24 mM )
* "≥" means soluble, but saturation unknown.
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.1724 mL | 5.8621 mL | 11.7242 mL |
| 5 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL |
| 10 mM | 0.1172 mL | 0.5862 mL | 1.1724 mL |
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (2.93 mM); Clear solution