2. Cell Cycle/DNA Damage Stem Cell/Wnt Apoptosis Epigenetics PI3K/Akt/mTOR
  3. Casein Kinase Survivin Epigenetic Reader Domain Akt Apoptosis Caspase MDM-2/p53
  4. CK2-TN03

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.

For research use only. We do not sell to patients.

CK2-TN03

CK2-TN03 Chemical Structure

CAS No. : 313226-24-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

CK2-TN03 Related Antibodies

Top Publications Citing Use of Products

View All Casein Kinase Isoform Specific Products:

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CK1 CK2

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Akt Akt1 Akt2 Akt3

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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[1].

IC50 & Target[1]

CK2

165 nM (IC50)

Caspase 3

 

Caspase-7

 

BRD4

 

Akt1

 

In Vitro

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.

CK2-TN03 Related Antibodies

Apoptosis Analysis[1]

Cell Line: Neuroblastoma CHP-212
Concentration: 0.35, 0.5 and 1.0 μM
Incubation Time: 48 h (monitored every 2 h)
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.

Cell Cycle Analysis[1]

Cell Line: Neuroblastoma CHP-212
Concentration: 0.5 and 1.0 μM
Incubation Time: 24 h, 48 h
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.

Cell Viability Assay[1]

Cell Line: Differentiated neuroblastoma SH-SY5Y
Concentration: 0.5 μM
Incubation Time: 48 h
Result: Did not reduce viability of differentiated SH-SY5Y cells, which had ~20% of the survivin protein levels present in undifferentiated cells.
In Vivo

CK2-TN03 (40 mg/kg; i.p.; once daily; 28 days) significantly reduces neuroblastoma xenograft tumor growth and improves mouse survival, with a subset of mice achieving long-term tumor control or remission[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: (Ncr)-Foxn1 nu nude mice (7-8 weeks old)[1]
Dosage: 40 mg/kg
Administration: i.p.; once daily; 28 days
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.
Molecular Weight

326.37

Formula

C17H14N2O3S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

Sequence

Asp-Lys-Phe-Val-Gly-{Leu-methyl}-{Nle}-NH2
Sequence Shortening

DKFVG-{Leu-methyl}-{Nle}-NH2
SMILES

COC(C=C1)=C(O)C=C1/C=C(C(N/2)=O)/SC2=N\C3=CC=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0640 mL 15.3200 mL 30.6401 mL
5 mM 0.6128 mL 3.0640 mL 6.1280 mL
View the 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.

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Purity & Documentation
References

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
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CK2-TN03 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CK2-TN03313226-24-3Casein KinaseSurvivinEpigenetic Reader DomainAktApoptosisCaspaseMDM-2/p53PKBProtein kinase BAKT1neuroblastoma cellsp53casein kinase 2survivinCK2αMDM2medulloblastoma DAOYBRD4MYCNInhibitorinhibitorinhibit

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