Casein Kinase Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S2248	Silmitasertib (CX-4945)	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.	Nat Cell Biol, 2025, 27(8):1272-1287 Nat Commun, 2025, 16(1):997 Metabolism, 2025, 162:156060
S0707	Silmitasertib (CX-4945) sodium salt	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'.	Diabetologia, 2024, 10.1007/s00125-024-06128-1 J Diabetes Investig, 2024, 15(6):684-692 Proc Natl Acad Sci U S A, 2022, 119(12):e2114336119
S7642	D 4476	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.	Neoplasia, 2025, 66:101175 Cell Rep Med, 2023, 4(4):101015 Cell Rep, 2023, 42(9):113035
S5265	TBB	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.	International Journal of Molecular Sciences, November 26, 2019, 5951 International Journal of Molecular Sciences, November 26, 2019, 5951 Nucleic Acids Research, December 2, 2019, 10977-10993
S8237	IC261	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.	Int J Nanomedicine, 2025, 20:9019-9030 Cell Rep, 2023, 42(7):112812 Cell Metab, 2022, S1550-4131(21)00542-8
S2249	PF 4800567	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).	Blood Advances, 2020, 3072-3084 Blood Advances, 2020, 3072-3084 Blood Adv, 2020, 4(13):3072-3084
S6734	PF-670462	PF-670462 is a potent and selective inhibitor of CK1ε and CK1δ with IC50 value of 90 nM and 13 nM, respectively.	NPJ Precis Oncol, 2025, 9(1):274 mSystems, 2025, 10(9):e0043825 J Biomed Sci, 2024, 31(1):72
S9850	(E/Z)-GO289	(E/Z)-GO289 potently and selectively inhibits casein kinase 2 (CK2) at an IC50 of 7 nM in vitro kinase assay.	Autophagy, 2024, 994-1014 Autophagy, 2023, 10.1080/15548627.2023.2281128
S6536	TTP 22	TTP22 is a casein kinase 2 (CK2) inhibitor with an IC50 value of 100 nM. It displays selectivity for CK2 over JNK3, ROCK1, and MET with no inhibitory effects towards these kinases at 10 μM.	Journal of Cell Biology, 2022, e202202100 J Cell Biol, 2022, 221-11e202202100
E2914	5,6-Dichlorobenzimidazole 1-beta-D-ribofuranoside	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.	Cancer Sci, 2025, 10.1111/cas.70081 Cancer Science, 2025, 1952-1962
S6578	Longdaysin	Longdaysin is a Casein Kinase inhibitor with IC50 values of 8.8 μM, 5.6 μM, 52 μM and 29 μM for CKIδ, CKIα, ERK2 and CDK7.	Nat Commun, 2021, 12(1):7003
S5516	Ellagic Acid hydrate	Ellagic acid is a potent inhibitor of protein kinase CK2 with IC50s of 0.04, 2.9 and 3.5 μM for CK2, Lyn and PKA respectively. It shows potent antioxidant, anti-mutagenic and antidepressant properties.	J Cell Biol, 2022, 221-11e202202100
S9331	7-Hydroxy-4-methyl-8-nitrocoumarin	7-Hydroxy-4-methyl-8-nitrocoumarin is a chemical.
E1455^New	BTX-A51	BTX-A51 (Casein Kinase inhibitor A51) is a first-in-class oral and potent inhibitor of casein kinase 1α (CK1α) and cyclin dependent kinase (CDK7/9) with an IC50 of 17 nM for CK1α and Kd of 1.3 nM and 4 nM for CDK7 and CDK9, respectively. It induces apoptosis of leukemic cells by activating p53 and inhibiting expression of Mcl1 and can be used in Acute myeloid leukemia (AML) cancer research.
S6544	SR-3029	SR-3029 is a potent and selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 values of 44 and 260 nM for CK1δ and CK1ε, respectively.
E7852	CKI-7	CKI-7 (CKI-7 2HCl) is an inhibitor of casein kinase 1 (CK1) with ki of 8.5 μM and IC50 of 6 μM. It is selective for CK1 over CK2, PKC, CaM kinase II (CaMKII), and cyclic AMP-dependent protein kinase (PKA) with IC50 of 90, >1000, 195, and 550 μM, respectively. This compound also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1).
E1927	PF-05251749（CK1-IN-2）	PF-05251749 (CK1-IN-2, Compound Nr.4) is a potent, selective, brain-penetrant inhibitor of Casein Kinase 1 (CK1) in a concentration-dependent manner, with IC50 values of 33.1 nM for CK1d and 51.6 nM for CK1e. It also functions as an inducer of CYP3A, with the potential to treat circadian rhythm disruptions in Alzheimer's and Parkinson's diseases.
S0350	CK1-IN-1	CK1-IN-1 (PUN51207, Compound 1C) is an inhibitor of casein kinase 1 (CK1) with IC50 of 15 nM, 16 nM and 73 nM for CK1δ, CK1ε and p38α MAPK, respectively.
E2659	DMAT	DMAT is a high affinity and selective casein kinase-2 (CK2) inhibitor with IC50 of ~0.14 μM and Ki of ~40 nM.
E2826	Hematein	Hematein inhibits casein kinase II activity in a selective, dose-dependent and ATP non-competitive manner in vitro, with IC50 of 0.55 μM in the presence of 10 μM ATP.
S0186	TA-01	TA-01 is a potent inhibitor of CK1δ/ε and p38 MAPK with IC50 of 6.4 nM, 6.8 nM and 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively.
S1105	LY294002	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.	Gut, 2025, gutjnl-2025-335163 Cell Mol Immunol, 2025, 22(5):541-556 Nat Commun, 2025, 16(1):1661
S7085	IWP-2	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.	Sci Bull (Beijing), 2025, S2095-9273(25)00472-4 Nat Commun, 2025, 16(1):1999 Nat Commun, 2025, 16(1):4688
S2805	LY364947	LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.	Adv Sci (Weinh), 2024, 11(4):e2304987 Cell Rep Med, 2024, 5(2):101416 Cell Commun Signal, 2024, 22(1):242
S0995	BioE-1115	BioE-1115 is a highly selective and potent dual inhibitor of PAS kinase (PASK) and casein kinase 2α (CK2α) with IC50 of ~4 nM and ~10 μM, respectively.