CX-4945

• CAT Number: I000112
• CAS Number: 1009820-21-6
• Molecular Formula: C₁₉H₁₂ClN₃O₂
• Molecular Weight: 349.77
• Purity: ≥95%
• Synonyms: 5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid
• Target: CK2
• Solubility: DMSO: ≥ 35mg/mL
• Storage: 3 years -20C powder
• IC50: 1 nM
• InChI: InChI=1S/C19H12ClN3O2/c20-12-2-1-3-13(9-12)22-18-15-6-7-21-10-16(15)14-5-4-11(19(24)25)8-17(14)23-18/h1-10H,(H,22,23)(H,24,25)
• InChIKey: MUOKSQABCJCOPU-UHFFFAOYSA-N
• SMILES: C1=CC(=CC(=C1)Cl)NC2=C3C=CN=CC3=C4C=CC(=CC4=N2)C(=O)O

CX-4945 (CAT: I000112) is a potent and selective inhibitor of protein kinase CK2 (casein kinase 2). CK2 is a serine/threonine protein kinase that plays a crucial role in regulating various cellular processes, including cell proliferation, survival, and apoptosis. CX-4945 specifically targets the ATP-binding site of CK2 and inhibits its kinase activity. By blocking CK2 activity, CX-4945 disrupts CK2-mediated signaling pathways involved in cancer progression and other diseases. Preclinical studies have shown that CX-4945 exhibits anti-proliferative and pro-apoptotic effects in cancer cells, making it a promising therapeutic agent for cancer treatment. Furthermore, CX-4945 has demonstrated efficacy in both in vitro and in vivo models of cancer, suggesting its potential for clinical application as an anticancer drug.

Reference

1:CX-4945: the protein kinase CK2 inhibitor and anti-cancer drug shows anti-fungal activity. Masłyk M, Janeczko M, Martyna A, Kubiński K.Mol Cell Biochem. 2017 May 13. doi: 10.1007/s11010-017-3068-z. [Epub ahead of print] PMID: 28501934 2:CX-4945, a selective inhibitor of casein kinase 2, synergizes with B cell receptor signaling inhibitors in inducing diffuse large B cell lymphoma cell death. Mandato E, Nunes SC, Zaffino F, Casellato A, Macaccaro P, Tubi LQ, Visentin A, Trentin L, Semenzato G, Piazza F.Curr Cancer Drug Targets. 2017 Apr 26. doi: 10.2174/1568009617666170427110450. [Epub ahead of print] PMID: 28460620 3:Targeting Protein Kinase CK2: Evaluating CX-4945 Potential for GL261 Glioblastoma Therapy in Immunocompetent Mice. Ferrer-Font L, Villamañan L, Arias-Ramos N, Vilardell J, Plana M, Ruzzene M, Pinna LA, Itarte E, Arús C, Candiota AP.Pharmaceuticals (Basel). 2017 Feb 12;10(1). pii: E24. doi: 10.3390/ph10010024. PMID: 28208677 Free PMC Article4:Autophagy Induced by CX-4945, a Casein Kinase 2 Inhibitor, Enhances Apoptosis in Pancreatic Cancer Cell Lines. Hwang DW, So KS, Kim SC, Park KM, Lee YJ, Kim SW, Choi CM, Rho JK, Choi YJ, Lee JC.Pancreas. 2017 Apr;46(4):575-581. doi: 10.1097/MPA.0000000000000780. PMID: 28196025 5:CK2 inhibitor CX-4945 destabilizes NOTCH1 and synergizes with JQ1 against human T-acute lymphoblastic leukemic cells. Lian H, Li D, Zhou Y, Landesman-Bollag E, Zhang G, Anderson NM, Tang KC, Roderick JE, Kelliher MA, Seldin DC, Fu H, Feng H.Haematologica. 2017 Jan;102(1):e17-e21. doi: 10.3324/haematol.2016.154013. Epub 2016 Oct 6. No abstract available. PMID: 27758824 Free PMC Article6:Synergistic cytotoxic effects of bortezomib and CK2 inhibitor CX-4945 in acute lymphoblastic leukemia: turning off the prosurvival ER chaperone BIP/Grp78 and turning on the pro-apoptotic NF-κB. Buontempo F, Orsini E, Lonetti A, Cappellini A, Chiarini F, Evangelisti C, Evangelisti C, Melchionda F, Pession A, Bertaina A, Locatelli F, Bertacchini J, Neri LM, McCubrey JA, Martelli AM.Oncotarget. 2016 Jan 12;7(2):1323-40. doi: 10.18632/oncotarget.6361. PMID: 26593250 Free PMC Article7:Different Persistence of the Cellular Effects Promoted by Protein Kinase CK2 Inhibitors CX-4945 and TDB. Girardi C, Ottaviani D, Pinna LA, Ruzzene M.Biomed Res Int. 2015;2015:185736. doi: 10.1155/2015/185736. Epub 2015 Oct 19. PMID: 26558259 Free PMC Article8:Micropillar arrays as potential drug screens: Inhibition of micropillar-mediated activation of the FAK-Src-paxillin signaling pathway by the CK2 inhibitor CX-4945. Kim J, Choi WJ, Moon SH, Jung J, Park JK, Kim SH, Lee JO.Acta Biomater. 2015 Nov;27:13-20. doi: 10.1016/j.actbio.2015.08.041. Epub 2015 Aug 28. PMID: 26318800 9:The casein kinase 2 inhibitor, CX-4945, as an anti-cancer drug in treatment of human hematological malignancies. Chon HJ, Bae KJ, Lee Y, Kim J.Front Pharmacol. 2015 Mar 31;6:70. doi: 10.3389/fphar.2015.00070. eCollection 2015. PMID: 25873900 Free PMC Article10:MEK inhibitor PD-0325901 overcomes resistance to CK2 inhibitor CX-4945 and exhibits anti-tumor activity in head and neck cancer. Bian Y, Han J, Kannabiran V, Mohan S, Cheng H, Friedman J, Zhang L, VanWaes C, Chen Z.Int J Biol Sci. 2015 Feb 23;11(4):411-22. doi: 10.7150/ijbs.10745. eCollection 2015. PMID: 25798061 Free PMC Article