Precision chemistryAug 27, 2026

An Oral Drug Based on a CK2 Inhibitor for Controlling Body Clock and Acute Myeloid Leukemia

Circadian Biology Weekly Brief ↗PubMed ↗DOI ↗OA ↗

Updated Aug 29, 2026

Abstract

The derivative GO847 demonstrated the ability to change cellular circadian rhythm periods and inhibit acute myeloid leukemia (AML) cell growth.

GO289 derivatives were developed to improve water solubility and metabolic stability for better in vivo applications.
GO847 showed effects on circadian rhythms and inhibited growth in AML cells similar to the original compound GO289.
Proteomic profiling indicated that GO847 and GO289 affect pathways related to mitochondrial function and known CK2 targets, including cell cycle and apoptosis.
Both compounds impaired the metabolic flexibility of mitochondria in AML cells.
After oral administration in mice, GO847 was found in plasma, liver, spleen, and bone marrow, but not in the brain.

Simplified

The protein kinase CK2 controls cell cycle, apoptosis, and circadian rhythms. The CK2 inhibitor CX-4945 is in clinical trials for cancer treatment, but it has many off-target proteins. Therefore, the development of a bioavailable and specific CK2 inhibitor has been awaited. We previously discovered a specific CK2 inhibitor, GO289, from cell-based phenotypic screening of circadian clock modulators. However, the low water solubility and metabolic stability of GO289 have limited in vivo applications. Here, we developed GO289 derivatives with higher water solubility and metabolic stability. A derivative, GO847, changed the period length of cellular circadian rhythms similar to GO289 and inhibited the growth of acute myeloid leukemia (AML) cells. A proteomic profiling suggested the effects of GO847 and GO289 on pathways related to mitochondrial function, in addition to well-known CK2 targets: cell cycle, apoptosis, RNA metabolism, and protein synthesis. Consistent with this observation, both compounds impaired the metabolic flexibility of mitochondria in AML cells. After oral administration to mice, GO847 was detected in the plasma, liver, spleen, and bone marrow but not in the brain. Together, the findings show that GO847 is a promising candidate for targeting AML, a malignant blood cancer that requires effective treatment.

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An Oral Drug Based on a CK2 Inhibitor for Controlling Body Clock and Acute Myeloid Leukemia

Abstract

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