ck1-in-1

CK1-IN-1 (PUN51207) is a casein kinase 1 (CK1) inhibitor. CK1-IN-1 has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively.

VRK1/CK1-IN-1 (compound 36) is a dual inhibitor targeting vaccinia-related kinase 1 (VRK1) and casein kinase 1 (CK1), with a Ki of 37.9 nM for VRK1. It exhibits IC50 values of 17 nM and 15 nM for CK1 δ and ε isoforms, respectively.

EGFRT790M/L858R/ACK1-IN-1 (Compound 21a) is a dual inhibitor targeting EGFRT790M/L858R and ACK1 with IC50 values of 23 nM and 263 nM, respectively. This compound effectively inhibits cell proliferation and exhibits antitumor activity.

CK1-IN-3 is casein kinase 1 (CK1) inhibitor and can be used for research on the treatment or prevention of diseases associated with circadiantiazol rhythm, inflammation diseases.

Epiblastin A is an inhibitor of Casein Kinase 1 (CK1). Epiblastin A engages CK1 isoenzymes in cell lysate and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs).

CK1δ-IN-10 (Compound 85) is an inhibitor of casein kinase 1 (CK1), specifically targeting CK1δ (CSNKID), with an IC50 value of 0.255 μM.

Casein kinase1δ-IN-27 (Compound 8) is an inhibitor of casein kinase 1 (CK1), effectively inhibiting CK1α, CK1δ, CK1ε, and p38α with IC50 values of 22, 16.5, 9.41, and 14.8 nM, respectively. It also suppresses DUX4 expression, with an IC50 of 10 nM.

CK1δ-IN-9 (Compound 8) is an inhibitor of casein kinase 1 (CK1), specifically targeting CK1δ with an IC50 of 1.4 nM. The compound also inhibits p38α and p38β with IC50 values of 0.25 μM and 0.78 μM, respectively. CK1δ-IN-9 exhibits favorable pharmacokinetic properties, including high oral bioavailability (70%) and moderate clearance.

Casein kinase1δ-IN-29 (Compound 18) is an inhibitor that targets p38α and casein kinase 1 (CK1), exhibiting inhibitory effects on p38α, CK1δ, and CK1ε with IC50 values of 0.041 µM, 0.005 µM, and 0.447 µM, respectively. This compound causes cell cycle arrest at the subG1 phase and induces apoptosis in AC1-M88 cells.

CK1γ-IN-1 is a non-selective inhibitor of CK1 kinases, exhibiting IC50 values of 780 nM, 570 nM, and 990 nM for human CK1γ1, CK1γ2, and CK1γ3, respectively. Its non-specific binding to various kinases potentially makes CK1γ-IN-1 useful for specific biological studies involving CK1γ.

D4476 (Casein Kinase I Inhibitor) is an effective, selective, and cell-permeant CK1 (casein kinase 1) inhibitor( IC50=300 nM in a cell-free assay).

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.

CK1tide serves as a substrate for Casein Kinase 1 (CK1), allowing for the assessment of CK1's catalytic activity in vitro by determining its ability to phosphorylate CK1tide.