dCK1α-2

dCK1α-2 is an **orally bioavailable small molecule molecular glue degrader** that selectively targets **casein kinase 1 alpha (CK1α)** for ubiquitin-mediated degradation via the **CRL4^CRBN E3 ubiquitin ligase complex**. The compound induces the formation of a ternary complex between CRBN and CK1α, leading to selective proteasomal degradation of CK1α, and as a result, modulates the **p53 signaling pathway**. dCK1α-2 shows potent anti-tumor activity in AML (acute myeloid leukemia) xenograft mouse models, is active in vitro and in vivo, displays high oral bioavailability (34% in mice), and upregulates p53 target gene expression post-CK1α degradation. It is a pharmacological tool compound under preclinical investigation as a targeted therapy for p53-dependent cancer settings[1][2][3][7].