ckiδ

SR-1277 is a potent, highly selective and ATP-competitive CK1δ ε inhibitor with IC50 values of 49 nM and 260 nM, respectively.CK1δ plays a crucial role in regulating Wee1 activity at the G2 M cell-cycle interface, and exhibits significant antiproliferative activity against a variety of cancer cells.

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.

MRT00033659 is an effective broad-spectrum kinase inhibitor of CK1 (IC50=0.9 µM for CK1δ) and CHK1 (IC50=0.23 µM). MRT00033659 is a pyrazolo-pyridine analogue. It also induces p53 pathway activation and E2F-1 destabilization.

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.

IC261 (SU-5607) is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.

TA-01 is a potent inhibitor of CK1 and p38 MAPK, with IC50 values of 6.4 nM for CK1ε, 6.8 nM for CK1δ, and 6.7 nM for p38 MAPK.

PF-4800567 is a selective inhibitor of casein kinase 1ε (CK1ε; IC50 = 32 nM) with greater than 20-fold selectivity over CK1δ.

Casein kinase 1δ-IN-3 (Compound 23a) is an inhibitor of casein kinase 1 delta (CK1δ) with a pIC50 of 6.5376 M.

Benazoline oxalate salt is a pharmacological active compound that inhibits casein kinase Iε (CKIε) or CKIδ phosphorylation of the PER2 protein.

CK1-IN-4 (Compound 59) is an inhibitor of casein kinase CK1δ with an IC50 of 2.74 μM. It exhibits neuroprotective activity in SH-SY5Y cells treated with Ethacrynic acid.