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Casein Kinase

Isoform-selective Products

Casein Kinase Products

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  • Casein Kinase Inhibitors (23)
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Catalog No. Product Name Information Product Use Citations Product Validations
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. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Signal Transduct Target Ther, 2024, 9(1):109
Signal Transduct Target Ther, 2024, 9(1):109
Nat Genet, 2024, 10.1038/s41588-024-01891-8
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, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.
Metabolism, 2025, 162:156060
Diabetologia, 2024, 10.1007/s00125-024-06128-1
Biomed Pharmacother, 2024, 180:117499
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.
Cell Stem Cell, 2024, S1934-5909(24)00256-X
Nat Commun, 2024, 15(1):1351
Nat Commun, 2024, 15(1):167
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
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
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.
Cell Rep Med, 2023, 4(4):101015
Cell Rep, 2023, 42(9):113035
Nat Commun, 2022, 13(1):3034
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.
Cell Rep, 2024, 43(2):113779
Mol Cell, 2023, 83(15):2792-2809.e9
Cancers (Basel), 2022, 15(1)200
S8237 IC261 IC261 (SU-5607) is a novel inhibitor of CK1. The IC50 of IC261 for CK1 is 16 μM and for Cdk5 is 4.5 mM.
Cell Rep, 2023, 42(7):112812
Cell Metab, 2022, S1550-4131(21)00542-8
Sci Rep, 2022, 12(1):7
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, 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.
J Cell Biol, 2022, 221-11e202202100
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
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 Adv, 2020, 4(13):3072-3084
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.
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.
E1413 DEG-77 DEG-77 is a cereblon-dependent degrader of IKZF2 and casein kinase 1α (CK1α). It blocks cell growth and delays leukemia progression in murine and human acute myeloid leukemia (AML) mouse models.
E1412 DEG-35 DEG-35 is a cereblon-dependent degrader of IKZF2 and casein kinase 1α (CK1α). It blocks cell growth and delays leukemia progression in murine and human acute myeloid leukemia (AML) mouse models.
S3143 Pyruvic acid

Pyruvic acid (Acetylformic acid) is an important organic chemical intermediate that plays a role in cardiomyocyte pathophysiology and therapy. Pyruvic acid markedly increases the level of lactate dehydrogenase (LDH) and creatine kinase (CK) and reduces the level of Ca2+Mg2+-ATPase and Na+K+-ATPase.
E1927New 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.
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.
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.
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.
J Biomed Sci, 2024, 31(1):72
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.
E2506 A-3 hydrochloride A-3 hydrochloride, a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases, againsts cAMP-dependent protein kinase (PKA) (Ki=4.3 µM), casein kinase II (CK2) (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM), also inhibits Protein Kinase C (PKC) and casein kinase I (CK1) with Ki values of 47 µM and 80 µM, respectively.
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. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Signal Transduct Target Ther, 2024, 9(1):109
Signal Transduct Target Ther, 2024, 9(1):109
Nat Genet, 2024, 10.1038/s41588-024-01891-8
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, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.
Metabolism, 2025, 162:156060
Diabetologia, 2024, 10.1007/s00125-024-06128-1
Biomed Pharmacother, 2024, 180:117499
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.
Cell Stem Cell, 2024, S1934-5909(24)00256-X
Nat Commun, 2024, 15(1):1351
Nat Commun, 2024, 15(1):167
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
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
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.
Cell Rep Med, 2023, 4(4):101015
Cell Rep, 2023, 42(9):113035
Nat Commun, 2022, 13(1):3034
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.
Cell Rep, 2024, 43(2):113779
Mol Cell, 2023, 83(15):2792-2809.e9
Cancers (Basel), 2022, 15(1)200
S8237 IC261 IC261 (SU-5607) is a novel inhibitor of CK1. The IC50 of IC261 for CK1 is 16 μM and for Cdk5 is 4.5 mM.
Cell Rep, 2023, 42(7):112812
Cell Metab, 2022, S1550-4131(21)00542-8
Sci Rep, 2022, 12(1):7
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, 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.
J Cell Biol, 2022, 221-11e202202100
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
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 Adv, 2020, 4(13):3072-3084
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.
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.
E1927New 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.
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.
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.
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.
J Biomed Sci, 2024, 31(1):72
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.
S3143 Pyruvic acid

Pyruvic acid (Acetylformic acid) is an important organic chemical intermediate that plays a role in cardiomyocyte pathophysiology and therapy. Pyruvic acid markedly increases the level of lactate dehydrogenase (LDH) and creatine kinase (CK) and reduces the level of Ca2+Mg2+-ATPase and Na+K+-ATPase.
E2506 A-3 hydrochloride A-3 hydrochloride, a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases, againsts cAMP-dependent protein kinase (PKA) (Ki=4.3 µM), casein kinase II (CK2) (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM), also inhibits Protein Kinase C (PKC) and casein kinase I (CK1) with Ki values of 47 µM and 80 µM, respectively.
E1927New 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.

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