CX-4945 (CAS 1009820-21-6)
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CX-4945 (Silmitasertib) is an ATP-competitive CK2 protein kinase inhibitor with a Ki and an IC50 of 0.38 and 1 nM for recombinant human CK2α, respectively. CX-4945 has broad-spectrum anti-proliferative activity in multiple cancer cell lines. The anti-proliferative activity of CX-4945 against cancer cells correlated with expression levels of the CK2α catalytic subunit. Attenuation of PI3K/Akt signaling by CX-4945 was evidenced by dephosphorylation of Akt on the CK2-specific S129 site and the canonical S473 and T308 regulatory sites. CX-4945 suppresses Akt signaling and inhibits proliferation of HUVEC Cells. CX-4945 causes cell-cycle arrest and selectively induced apoptosis in certain cancer cells. In models of angiogenesis, CX-4945 inhibited human umbilical vein endothelial cell migration, tube formation, and blocked CK2-dependent hypoxia-induced factor 1 alpha (HIF-1α) transcription in cancer cells. Collectively, CX-4945 inhibits pro-angiogenic CK2 signaling in vitro and in vivo.
CX-4945 (CAS 1009820-21-6) References
- CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. | Siddiqui-Jain, A., et al. 2010. Cancer Res. 70: 10288-98. PMID: 21159648
- Effects of the CK2 inhibitors CX-4945 and CX-5011 on drug-resistant cells. | Zanin, S., et al. 2012. PLoS One. 7: e49193. PMID: 23145120
- CK2 inhibitor CX-4945 blocks TGF-β1-induced epithelial-to-mesenchymal transition in A549 human lung adenocarcinoma cells. | Kim, J. and Hwan Kim, S. 2013. PLoS One. 8: e74342. PMID: 24023938
- CX-4945: the protein kinase CK2 inhibitor and anti-cancer drug shows anti-fungal activity. | Masłyk, M., et al. 2017. Mol Cell Biochem. 435: 193-196. PMID: 28501934
- CX-4945 Induces Methuosis in Cholangiocarcinoma Cell Lines by a CK2-Independent Mechanism. | Lertsuwan, J., et al. 2018. Cancers (Basel). 10: PMID: 30142881
- Casein Kinase 2 Inhibitor, CX-4945, as a Potential Targeted Anticancer Agent in Gastric Cancer. | Kim, HM., et al. 2018. Anticancer Res. 38: 6171-6180. PMID: 30396934
- Influence of Casein kinase II inhibitor CX-4945 on BCL6-mediated apoptotic signaling in B-ALL in vitro and in vivo. | Richter, A., et al. 2020. BMC Cancer. 20: 184. PMID: 32131762
- Role of CK2 inhibitor CX-4945 in anti-cancer combination therapy - potential clinical relevance. | D'Amore, C., et al. 2020. Cell Oncol (Dordr). 43: 1003-1016. PMID: 33052585
- CX-4945 and siRNA-Mediated Knockdown of CK2 Improves Cisplatin Response in HPV(+) and HPV(-) HNSCC Cell Lines. | Trembley, JH., et al. 2021. Biomedicines. 9: PMID: 34070147
- Sequence of CX-4945 and Cisplatin Administration Determines the Effectiveness of Drug Combination and Cellular Response in Cholangiocarcinoma Cells In Vitro. | Lertsuwan, J., et al. 2021. Anticancer Res. 41: 6155-6167. PMID: 34848470
- Anti-Growth, Anti-Angiogenic, and Pro-Apoptotic Effects by CX-4945, an Inhibitor of Casein Kinase 2, on HuCCT-1 Human Cholangiocarcinoma Cells via Control of Caspase-9/3, DR-4, STAT-3/STAT-5, Mcl-1, eIF-2α, and HIF-1α. | Wang, S., et al. 2022. Int J Mol Sci. 23: PMID: 35683032
- The Casein Kinase 2 Inhibitor CX-4945 Promotes Cholangiocarcinoma Cell Death Through PLK1. | Lee, DS., et al. 2022. Anticancer Res. 42: 3435-3443. PMID: 35790285
- Anti-adipogenic and Pro-lipolytic Effects on 3T3-L1 Preadipocytes by CX-4945, an Inhibitor of Casein Kinase 2. | Yadav, AK. and Jang, BC. 2022. Int J Mol Sci. 23: PMID: 35806278
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
CX-4945, 2 mg | sc-364475 | 2 mg | $183.00 | |||
CX-4945, 50 mg | sc-364475A | 50 mg | $800.00 |