CK1 inhibitor

Ack1 inhibitor 1 is a potent and selective orally active inhibitor of ACK1 kinase, with an IC50 value of 2.1 nM. It effectively inhibits the phosphorylation of ACK1 and the activation of downstream AKT, demonstrating anti-tumor activity [1].

Ack1 Inhibitor 2, also referred to as Example 259, effectively inhibits Ack1 with an IC50 value of 0.46 μM [1].

TBCA (Casein Kinase II Inhibitor III, TBCA) is a highly selective CK2 (casein kinase II) inhibitor, IC50 = 110 nM, Ki = 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases.

CKI-7 is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. It also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

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).

CKI-7 free base is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor, also inhibiting SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It inhibits PKC and casein kinase I with Ki values of 47 μM and 80 μM, respectively[1], and also inhibits PKA (Ki=4.3 μM), casein kinase II (Ki=5.1 μM), and myosin light chain kinase (MLCK) (Ki=7.4 μM).

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.

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.

JW 67 is an inhibitor of canonical Wnt pathway signaling. JW 67 rapidly reduced active β-catenin with a subsequent downregulation of Wnt target genes, including AXIN2, SP5, and NKD1.

cdk CK1 inhibitor,potent and ATP-competitive

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.

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).

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.

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.

5-Iodotubercidin (NSC-113939) is a potent adenosine kinase inhibitor with IC50 of 26 nM. It inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.

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.

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.

CK1-IN-2 (compound Nr.4) hydrochloride is an effective inhibitor of CK1, exhibiting inhibitory IC50 values of 123 nM, 19.8 nM, 26.8 nM, and 74.3 nM against CK1a, CK1d, CK1e, and p38a respectively.