| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
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| 10mg |
|
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| 50mg |
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| Other Sizes |
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| Targets |
NEDD8 activating enzyme (NAE)[1]
|
|---|---|
| ln Vitro |
With IC50s of 100 and 122 nM, respectively, ZM223 hydrochloride (0.1–1 μM; 4 hours) inhibits HCT-116 and U-2OS cancer cells[1]. The administration of ZM223 hydrochloride (0.1–1 μM) for four hours results in a dose-dependent reduction in NEDD8 levels and an accumulation of UBC12 protein, which suggests a decrease in the NEDD8-UBC12 complex that follows[1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: HCT116 colon cancer cells and U-2OS osteosarcoma cells Tested Concentrations: 0.1 μM, 1 μM Incubation Duration: 4 hrs (hours) Experimental Results: Inhibited both HCT-116 and U-2OS cancer cells. Western Blot Analysis[1] Cell Types: HCT116 colon cancer cells Tested Concentrations: 0.1 μM, 1 μM Incubation Duration: 4 hrs (hours) Experimental Results: Caused a decrease in the level of NEDD8 and an increase in the downstream UBC12 protein. |
| References |
| Molecular Formula |
C23H18CLF3N4O2S2
|
|---|---|
| Molecular Weight |
538.992831707001
|
| Exact Mass |
538.051
|
| CAS # |
2438679-27-5
|
| Related CAS # |
ZM223;2031177-48-5
|
| PubChem CID |
139035004
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
35
|
| Complexity |
713
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
DXCZCDSLNIYJQF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H17F3N4O2S2.ClH/c24-23(25,26)14-3-1-13(2-4-14)21(32)30-22-29-18-10-7-16(11-19(18)34-22)28-20(31)12-33-17-8-5-15(27)6-9-17;/h1-11H,12,27H2,(H,28,31)(H,29,30,32);1H
|
| Chemical Name |
N-[6-[[2-(4-aminophenyl)sulfanylacetyl]amino]-1,3-benzothiazol-2-yl]-4-(trifluoromethyl)benzamide;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 150 mg/mL (278.30 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (13.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 75.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 7.5 mg/mL (13.91 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 75.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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