| S7085 |
IWP-2
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IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM in a cell-free assay, selective blockage of Porcn-mediated Wnt palmitoylation, does not affect Wnt/β-catenin in general and displays no effect against Wnt-stimulated cellular responses. IWP-2 specifically inhibits CK1δ.
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Cell Metab, 2026, 38(4):673-693.e17
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Gut Microbes, 2026, 18(1):2639216
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Sci Bull (Beijing), 2025, S2095-9273(25)00472-4
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| S1105 |
LY294002
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LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. This compound also inhibits CK2 with IC50 of 98 nM. It is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
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Research (Wash D C), 2026, 9:1190
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Cell Prolif, 2026, 59(3):e70108
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EMBO Rep, 2026, 27(5):1270-1300
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| S2248 |
Silmitasertib (CX-4945)
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Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, although it is less potent against Flt3, Pim1 and CDK1 (inactive in cell-based assay). This compound induces autophagy and promotes apoptosis. Phase 1/2.
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Theranostics, 2026, 16(7):3648-3664
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Nat Cell Biol, 2025, 27(8):1272-1287
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Nat Commun, 2025, 16(1):997
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| S0707 |
Silmitasertib (CX-4945) sodium salt
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Silmitasertib (CX-4945) sodium salt is a potent, orally bioavailable and selective inhibitor of casein kinase 2 (CK2) with IC50 of 1 nM against CK2α and CK2α'.
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CNS Neuroscience & Therapeutics, April 14 2022, 28(7):1033-1044
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Cancer Research, April 03 2025, 85(7):1253-1269
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Diabetologia, 2024, 10.1007/s00125-024-06128-1
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| S7642 |
D 4476
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D 4476 is a potent, selective, and cell-permeant CK1 (casein kinase 1) inhibitor with IC50 of 200 nM and 300 nM in a cell-free assay for CK1 from Schizosaccharomyces pombe and CK1δ, respectively. Also acts as an ALK5 inhibitor with IC50 of 500 nM.
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Neoplasia, 2025, 66:101175
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Cell Rep Med, 2023, 4(4):101015
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Cell Rep, 2023, 42(9):113035
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| S5265 |
TBB
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TBB (4,5,6,7-tetrabromobenzotriazole) is a selective cell-permeable CK2 inhibitor with IC50 values of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively.
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International Journal of Molecular Sciences, November 26, 2019, 5951
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International Journal of Molecular Sciences, November 26, 2019, 5951
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Nucleic Acids Research, December 2, 2019, 10977-10993
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| S8237 |
IC261
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IC261 (SU-5607) is a novel inhibitor of CK1. The IC50 of this compound for CK1 is 16 μM and for Cdk5 is 4.5 mM.
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Int J Nanomedicine, 2025, 20:9019-9030
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Cell Rep, 2023, 42(7):112812
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Cell Metab, 2022, S1550-4131(21)00542-8
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| S6734 |
PF-670462
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PF-670462 is a potent and selective inhibitor of CK1ε and CK1δ with IC50 value of 90 nM and 13 nM, respectively.
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NPJ Precis Oncol, 2025, 9(1):274
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mSystems, 2025, 10(9):e0043825
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J Biomed Sci, 2024, 31(1):72
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| S2249 |
PF 4800567
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PF 4800567 is a novel and potent inhibitor of casein kinase 1 epsilon (IC50=32 nM) with greater than 20-fold selectivity over casein kinase 1 delta(IC50=711 nM).
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Blood Advances, July 14, 2020, 3072-3084
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Sci Adv, 2026, 12(17):eadw4136
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Blood Advances, 2020, 3072-3084
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| E2914 |
5,6-Dichlorobenzimidazole 1-beta-D-ribofuranoside
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5,6-Dichlorobenzimidazole riboside(DRB) is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II and CDKs. It trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells.
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Cell Rep Methods, 2026, S2667-2375(26)00080-9
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Cancer Science, 2025, 1952-1962
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Cancer Sci, 2025, 10.1111/cas.70081
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