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Description: Potent and selective CK2α and CK2α' inhibitor. Also blocks CK2-dependent HIF-1α transcription, causes cell-cycle arrest, induces apoptosis in cancer cells and induces stem cell reprogramming
Alternative Names: Silmitasertib
Chemical Name: Sodium 5-[(3-Chlorophenyl)amino]benzo[c]-2,6-naphthyridine-8-carboxylate
Purity: ≥98% (HPLC)
Biological Activity for CX-4945
CX-4945 (Silmitasertib) is a potent and selective inhibitor of protein kinase CK2α and CK2α' (IC50 = 1 nM). It shows greater than 500-fold selectivity for CK2 over a panel of > 200 kinases.
CX-4945 can be used, in combination with other small molecules, in fast chemical reprogramming protocols for the induction of human somatic cells and highly efficient generation of pluripotent stem cells (hCiPS) in a minimum of 16 days with robust repeatability and reliability.
CX-4945 has antiproliferative effects in vitro as it attenuates PI3K/Akt signalling, causes cell-cycle arrest and selectively induces apoptosis in cancer cells. In models of angiogenesis, CX-4945 inhibits human umbilical vein endothelial cell migration, tube formation, and blocks CK2-dependent hypoxia-induced factor 1 alpha (HIF-1α) transcription in cancer cells.
In vivo, CX-4945 displays robust antitumor activity with concomitant reduction of the mechanism-based biomarker phospho-p21 (T145) (murine xenograft model). CX-4945 is orally bioavailable.
Technical Data for CX-4945
| M. Wt | 371.76 |
| Formula | C19H11ClN3O2Na |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1309357-15-0 |
| InChI Key | ODDAAPQSODILSN-UHFFFAOYSA-M |
| Smiles | O=C(C1=CC(N=C(C2=C3C=NC=C2)NC4=CC(Cl)=CC=C4)=C3C=C1)O[Na] |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CX-4945
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 37.18 | 100 | |
| DMSO | 37.18 | 100 |
Preparing Stock Solutions for CX-4945
The following data is based on the product molecular weight 371.76. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.69 mL | 13.45 mL | 26.9 mL |
| 5 mM | 0.54 mL | 2.69 mL | 5.38 mL |
| 10 mM | 0.27 mL | 1.34 mL | 2.69 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets for CX-4945
References for CX-4945
References are publications that support the biological activity of the product.
Siddiqui-Jain et al (2010) CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Res. 70 10288 PMID: 21159648
Liuyang et al (2023) Highly efficient and rapid generation of human pluripotent stem cells by chemical reprogramming. Cell Stem Cell 30 450 PMID: 36944335
Wang et al (2025) A rapid chemical reprogramming system to generate human pluripotent stem cells. Nat.Chem.Biol. 21 1030 PMID: 39753706
If you know of a relevant reference for CX-4945, please let us know.
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Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
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- Chemotherapy Targets