ckiα

Longdaysin is an inhibitor of CK1α and CK1δ (IC50s: 5.6 8.8 µM). It also can inhibit ERK2 (IC50: 52 µM).

NCC007 is a novel CKIα and CKIδ dual inhibitors by structural modification of N9 and C2 position of longdaysin.

LH846 is a selective inhibitor of CK1δ with IC50 values of 290 nM for CK1δ, 1.3 μM for CK1ε, and 2.5 μM for CK1α, and exhibits no inhibitory activity at CK2.

BTX161 is a Thalidomide analogue. BTX161 is a potent CKIα degrader. In human AML cells, BTX161 mediates the CKIα degradation better than Lenalidomide as well as activates DNA damage response (DDR) and p53, and also stabilizes the p53 antagonist MDM2[1].

CK1-IN-2 (compound Nr.4) is a potent CK1 inhibitor with IC50 values of 123, 19.8, 26.8, and 74.3 nM for CK1a, CK1d, CK1e, and p38a, respectively, and is used in DUX4 overexpression-associated diseases, such as muscular dystrophy.