Light in the Dark (proteome)
Uncovering the dark kinome is one of the current challenges in life science research. The chemical probe CK156 provides the scientific community with a powerful tool to elucidate the role of DRAK1, a member of the DAPK family, in health and disease.
The chemical probe CK156 with its high selectivity towards DRAK1 (KD=21 nM as determined by ITC) will shed light on this part of the dark kinome. The potency in cells and its cellular target engagement amounts to 181 nM in intact cells, and 69 nM in lysed cells (IC50s), respectively.
CK156 has been made available to the research community through EUbOPEN and will encourage researchers to further explore the role of DRAK1 in human diseases, especially in cancer.
Figure. Left panel: Binding mode of CK156 in DRAK1 (PDB 7QUF). Right panel: NanoBRET assay for off-targets, identified in a kinome wide screen (DiscoverX).
For more information about the CK156 chemical probe visit the SGC website.