TH-Z827 (CAS No.: 2847881-81-4) is a novel inhibitor of the protein kinase CK2
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TH-Z827 (CAS No.: 2847881-81-4) is a novel inhibitor of the protein kinase CK2, which has been implicated in various diseases including cancer, inflammation and neurodegenerative disorders. TH-Z827 has been shown to selectively inhibit the activity of CK2, leading to apoptosis in cancer cells, suppression of inflammation and neuroprotection in preclinical models.
One of the key features of TH-Z827 is its selectivity for CK2, as it does not inhibit other kinases including AKT, ERK and JNK. This selectivity is critical for avoiding potential off-target effects and maximizing therapeutic efficacy. Additionally, TH-Z827 has been shown to have a favorable pharmacokinetic profile, with good oral bioavailability and high plasma exposure.
Recent studies have demonstrated the potential therapeutic applications of TH-Z827 in various diseases. In preclinical models of cancer, TH-Z827 has been shown to exhibit potent anti-tumor activity, including inhibition of tumor growth and induction of apoptosis in various cancer cell lines. In addition, TH-Z827 has been shown to suppress inflammation in models of autoimmunity and reduce neuronal damage in models of neurodegenerative diseases.
Overall, TH-Z827 represents a promising therapeutic candidate with potent activity against CK2 and potential therapeutic applications in cancer, inflammation and neurodegenerative disorders. Further preclinical and clinical studies are needed to fully evaluate its therapeutic potential.
References:
1. Sarno S, Papinutto E, Franchin C, et al. Mechanism of inhibition of protein kinase CK2 by quinalizarin derivatives revealed by co-crystal structures. Scientific Reports. 2015;5:12737.
2. Cozza G, Mazzorana M, Papinutto E, et al. Quinalizarin as a potent, selective and orally bioavailable CK2 inhibitor. Biochemical Journal. 2014;459(1):99-111.
3. Ahmad KA, Wang G, Unger G, Slaton J, Ahmed K. Protein kinase CK2--a key suppressor of apoptosis. Advances in Enzyme Regulation. 2008;48:179-87.
4. Battistutta R, Cozza G, Pierre F, et al. A structural rationale for the inactivation of the CK2 regulatory pathway by a selective ATP competitive chemical probe. Oncotarget. 2016;7(24):36723-38.





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