[CAS NO. 2438679-27-5] ZM223 hydrochloride
PRODUCTS SPECIFICATIONS [2438679-27-5]
DESCRIPTION [2438679-27-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 538.99 |
| Molecular Formula | C23H18ClF3N4O2S2 |
| SMILES | O=C(C1=CC=C(C(F)(F)F)C=C1)NC2=NC3=CC=C(NC(CSC4=CC=C(N)C=C4)=O)C=C3S2.[H]Cl |
Summary
ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme ( NAE ) inhibitor with excellent anticancer activity [1] .
IC50 & Target
NEDD8 activating enzyme (NAE) [1]
In Vitro
ZM223 hydrochloride (0.1-1 μM; 4 hours) inhibits both HCT-116 and U-2OS cancer cells with IC
50
s of 100 and 122 nM, respectively
[1]
.
ZM223 hydrochloride (0.1-1 μM; 4 hours) causes a dose-response decrease in the level of NEDD8 and accumulation of the UBC12 protein, indicating the decrease of the subsequent NEDD8-UBC12 complex
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | HCT116 colon cancer cells and U-2OS osteosarcoma cells |
| Concentration: | 0.1 μM, 1 μM |
| Incubation Time: | 4 hours |
| Result: | Inhibited both HCT-116 and U-2OS cancer cells. |
Western Blot Analysis [1]
| Cell Line: | HCT116 colon cancer cells |
| Concentration: | 0.1 μM, 1 μM |
| Incubation Time: | 4 hours |
| Result: | Caused a decrease in the level of NEDD8 and an increase in the downstream UBC12 protein. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 150 mg/mL ( 278.30 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8553 mL | 9.2766 mL | 18.5532 mL |
| 5 mM | 0.3711 mL | 1.8553 mL | 3.7106 mL |
| 10 mM | 0.1855 mL | 0.9277 mL | 1.8553 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 7.5 mg/mL (13.91 mM); Suspended solution; Need ultrasonic