CK2-TN03
Based on 1 Customer Validation
CK2-TN03 is an ATP-competitive casein kinase 2 (CK2) inhibitor, with an IC50 of 165 nM and a Ki of 20 nM. CK2-TN03 inhibits CK2-mediated survivin activation and reduces CK2-dependent phosphorylation levels of BRD4/MYCN and AKT1. CK2-TN03 exerts anti-neuroblastoma effects by inhibiting survivin, leading to mitotic catastrophe and apoptosis of cancer cells. CK2-TN03 can be used in studies related to neuroblastoma.
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- Pureté: 98.02%
- CAS No.: 313226-24-3
- Formule: C17H14N2O3S
- Masse moléculaire:326.37
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
|
CK2 165 nM (IC50) |
Caspase 3 |
Caspase-7 |
BRD4 |
Akt1 |
CK2-TN03 (0.2-25.0 μM; 48 h) induces dose-dependent cell death in the medulloblastoma DAOY cell line and multiple neuroblastoma cell lines, with EC50 values ranging from 0.31 to 1.95 μM; it shows no activity in glioblastoma U87 cells (EC50 >25 μM)[1].
CK2-TN03 (0.35-1.0 μM; 48 h) activates caspase 3/7 in CHP-212 neuroblastoma cells in a time-dependent manner, and primarily induces caspase-dependent apoptosis[1].
CK2-TN03 (0.5-1.0 μM; 24-48 h) induces G2/M cell cycle arrest and subsequent cell death in CHP-212 neuroblastoma cells[1].
CK2-TN03 (0.5 μM; 24 h) arrests CHP-212 neuroblastoma cells in mitosis, blocks successful cell division, and induces mitotic catastrophe and cell death[1].
CK2-TN03 (0.5 μM; 48 h) downregulates the activity and expression of survivin in CHP-212 neuroblastoma cells by directly inhibiting CK2-mediated phosphorylation of survivin and indirectly altering the AKT1/MDM2/p53 and BRD4/MYCN pathways, without changing the expression of CK2[1].
CK2-TN03 (0.5 μM; 48 h) does not affect the viability of differentiated quiescent SH-SY5Y neuroblastoma cells, which exhibit low survivin expression levels[1].
CK2-TN03 (1-10 μM; 72 h) induces cell death in a diverse panel of 160 cancer cell lines, with significant tumor entity selectivity, and exhibits the highest potency against melanoma, lymphoma, lung cancer, neuroblastoma, ovarian cancer, myeloma, soft tissue cancer and osteosarcoma cell lines[1].
CK2-TN03 (10 μM; 1 h) exhibits excellent permeability in MDCKII-MDR1 cells, with negligible efflux and no P-gp substrate activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Neuroblastoma CHP-212
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Concentration:0.35, 0.5 and 1.0 μM
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Incubation Time:48 h (monitored every 2 h)
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Result:Induced a time-dependent increase in caspase 3/7 activation, with significantly higher activation levels observed from 18 h onward compared to vehicle-treated controls.
Left a fraction of cell death unaffected by cotreatment with pan-caspase inhibitor Q-VD-OPh, while the inhibitor reduced most CK2-TN03-induced cell death.
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Cell Line:Neuroblastoma CHP-212
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Concentration:0.5 and 1.0 μM
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Incubation Time:24 h, 48 h
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Result:Increased the percentage of cells in the G2/M phase and the subG1 (dead cell) population after 24 and 48 h of treatment, with significant increases observed at both concentrations and time points compared to controls.
Increased G2/M phase cells after 24 h at 0.5 μM and 1.0 μM.
Further elevated G2/M and subG1 populations after 48 h at both concentrations.
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Cell Line:Differentiated neuroblastoma SH-SY5Y
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Concentration:0.5 μM
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Incubation Time:48 h
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Result:Did not reduce viability of differentiated SH-SY5Y cells, which had ~20% of the survivin protein levels present in undifferentiated cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:(Ncr)-Foxn1 nu nude mice (7-8 weeks old)[1]
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Dosage:40 mg/kg
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Administration:i.p.; once daily; 28 days
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Result:Reduced tumor growth rate, with tumor volume relative to baseline (VTx/VT0) reaching ~6 on day 28, compared to ~9 in vehicle controls.
Improved mouse survival: 5 treated mice survived to day 49, compared to 1 vehicle-treated mouse; 2 treated mice survived beyond day 85, with one showing complete tumor remission by day 14 and the other exhibiting a small, non-growing tumor mass post-treatment.
Increased p53 levels and decreased survivin levels and survivin phosphorylation in tumor tissue.
Chemical Information
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CAS No. 313226-24-3
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Appearance Solid
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Masse moléculaire 326.37
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Formule C17H14N2O3S
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Color Light yellow to yellow
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SMILES
COC(C=C1)=C(O)C=C1/C=C(C(N/2)=O)/SC2=N\C3=CC=CC=C3
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Sequence
Asp-Lys-Phe-Val-Gly-{Leu-methyl}-{Nle}-NH2
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Sequence Shortening
DKFVG-{Leu-methyl}-{Nle}-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 83.33 mg/mL (255.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (280 KB)
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SDS (252 KB)
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- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0640 mL | 15.3200 mL | 30.6401 mL | 76.6002 mL |
| 5 mM | 0.6128 mL | 3.0640 mL | 6.1280 mL | 15.3200 mL | |
| 10 mM | 0.3064 mL | 1.5320 mL | 3.0640 mL | 7.6600 mL | |
| 15 mM | 0.2043 mL | 1.0213 mL | 2.0427 mL | 5.1067 mL | |
| 20 mM | 0.1532 mL | 0.7660 mL | 1.5320 mL | 3.8300 mL | |
| 25 mM | 0.1226 mL | 0.6128 mL | 1.2256 mL | 3.0640 mL | |
| 30 mM | 0.1021 mL | 0.5107 mL | 1.0213 mL | 2.5533 mL | |
| 40 mM | 0.0766 mL | 0.3830 mL | 0.7660 mL | 1.9150 mL | |
| 50 mM | 0.0613 mL | 0.3064 mL | 0.6128 mL | 1.5320 mL | |
| 60 mM | 0.0511 mL | 0.2553 mL | 0.5107 mL | 1.2767 mL | |
| 80 mM | 0.0383 mL | 0.1915 mL | 0.3830 mL | 0.9575 mL | |
| 100 mM | 0.0306 mL | 0.1532 mL | 0.3064 mL | 0.7660 mL |