Caseína quinasa

CK1δ-IN-3 (compound 376) is a CK1δ (casein kinase 1δ) inhibitor that can be used to study neurodegenerative diseases such as Alzheimer's disease.

CX-5279 is a potent and selective CK2 inhibitor, exhibiting IC50 values of 2.73 nM for nCK2 and 0.91 nM for CK2α. It shows sensitivity to mutations Val66, Ile174, and V66I174AA, with IC50 values of 13.8 nM, 12.5 nM, and 23.35 nM, respectively, and demonstrates weak inhibitory activity against PIM1 with an IC50 of 8.52 μM. CX-5279 displays antiproliferative activity across various cancer cell lines and can be used in research on cancers such as pancreatic cancer and leukemia.

GSK-3β/CK-1δ-IN-1 (8d) is a dual inhibitor of GSK-3β and CK-1δ that can cross the blood-brain barrier, with IC50 values of 0.77 μM and 0.57 μM, respectively. GSK-3β/CK-1δ-IN-1 (8d) is applicable in neuroblastoma research.

IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDAC. It exhibits high selectivity for CK2 with an IC50 of 1.7 nM and demonstrates broad inhibitory activity against HDAC (HDAC1, 2, 3, and 6) with IC50 values of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, while showing low activity against HDAC8. IOR-160 modulates critical cell signaling pathways by inhibiting AKT phosphorylation and increasing α-tubulin acetylation. The compound reduces tumor growth and burden through its dual inhibition of CK2/HDAC and is relevant for research on triple-negative breast cancer.

CK2-IN-7 (compound 2), a casein kinase 2 (CK2) inhibitor, demonstrates a synergistic effect when used in combination with a structurally distinct CK2 chemical probe, SGC-CK2-1, in targeting cancer ^[1].

BMS-135 is a potent and selective ATP-competitive inhibitor of casein kinase 2 (CK2), with IC50 values of 0.8 nM for CK2α and 0.3 nM for CK2α' isoforms. It mimics the structure of ATP, binding to the active site of CK2 and inhibiting its serine/threonine phosphorylating activity. BMS-135 effectively inhibits cell proliferation and demonstrates antitumor properties, making it useful for research in colon cancer.

CK1δ-IN-1 (example 939) is an inhibitor of casein kinase 1δ (CK1δ). CK1δ-IN-1 is utilized for research in Alzheimer's disease.

CK2 inhibitor4 (compound 5b) is a protein kinase CK2 inhibitor with an IC₅₀ of 3.8 μM. It is applicable in tumor research.

CK2 Inhibitor 2, characterized as a potent, selective, and orally active inhibitor of CK2, demonstrates an impressive IC50 value of 0.66 nM.

AMG-548 hydrochloride: orally active, p38α inhibitor (Ki=0.5 nM), 1000x less for p38γ/δ, also blocks TNFα (IC50=3 nM) & inhibits casein kinase 1 δ/ε.

AMG-548 dihydrochloride, an oral p38α inhibitor (Ki: 0.5 nM), selectively targets p38β, γ, δ, inhibits TNFα (IC50: 3 nM), and suppresses Wnt signaling.