| MDL | - |
|---|---|
| Molecular Weight | 861.47 |
| Molecular Formula | C48H57ClN8O5 |
| SMILES | O=C(C(C=CC1=C2Cl)=CC1=NC3=C2CCCC3)NCCC[C@@H](CC4=CC=CC=C4)C(N5CCC(CN6C=NC7=C(C=CC(NC(CCN8CCN(C)CC8)=O)=C7)C6=O)(O)CC5)=O |
XL177A is a potent USP7 inhibitor and p53 stabilizer in cyto. XL177A suppresses cancer cell growth predominantly through a p53-dependent mechanism. XL177A labels the catalytic cysteine, C223, of USP7 with exquisite selectivity for USP7 across the DUBome and human proteome
[1]
.
XL177A (1 μM) induces complete G1 arrest in MCF7 cells after 24 hours
[1]
.
Treatment of MCF7 cells, which express WT TP53, with XL177A (0.001- 10 μM) induces rapid degradation of HDM2 within 2 hours, followed by increases in p53 and downstream p21 protein levels
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | MCF7 cells |
| Concentration: | 0.001, 0.01, 0.1, 1, 10 μM |
| Incubation Time: | 18-24 hours |
| Result: | The p53 and p21 protein levels remained high, but MDM2 protein levels matched DMSO control. |
Solid
Room temperature in continental US; may vary elsewhere.
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
DMSO : 25 mg/mL ( 29.02 mM ; Need ultrasonic)
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.1608 mL | 5.8040 mL | 11.6081 mL |
| 5 mM | 0.2322 mL | 1.1608 mL | 2.3216 mL |
| 10 mM | 0.1161 mL | 0.5804 mL | 1.1608 mL |
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.41 mM); Clear solution