Casein Kinase

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Casein Kinase Products

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Catalog No. Product Name Information Product Use Citations Product Validations
E2826New 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.
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.
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'.
Proc Natl Acad Sci U S A, 2022, 119(12):e2114336119
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00003-0
Int J Mol Sci, 2022, 23(8)4409
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.
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.
Immunity, 2022, 55(1):159-173.e9
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.2292.2021
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.
Mol Cell, 2022, S1097-2765(22)00394-X
EMBO Rep, 2022, e54801
Proc Natl Acad Sci U S A, 2022, 119(12):e2114336119
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
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.
Cell Rep, 2022, 38(5):110329
Front Immunol, 2022, 13:853894
Aging Dis, 2022, 13(1):313-328
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.
J Proteome Res, 2022, 21(4):1073-1082
bioRxiv, 2021, 10.1101/2021.03.17.435124
Commun Biol, 2021, 4(1):336
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.
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.
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.
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
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.
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, 2022, 29(4):545-558.e13
Adv Sci (Weinh), 2022, e2104299
Nat Commun, 2022, 13(1):2387
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.
Nat Commun, 2022, 13(1):3034
J Cell Biol, 2022, 221(1)e202103033
Adv Sci (Weinh), 2021, e2004846
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 Metab, 2022, S1550-4131(21)00542-8
Sci Rep, 2022, 12(1):7
EMBO Rep, 2021, e51503
S9850New (E/Z)-GO289

(E/Z)-GO289 potently and selectively inhibits casein kinase 2 (CK2) at an IC50 of 7 nM in vitro kinase assay.

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.

E2826New 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.
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.
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'.
Proc Natl Acad Sci U S A, 2022, 119(12):e2114336119
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00003-0
Int J Mol Sci, 2022, 23(8)4409
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.
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.
Immunity, 2022, 55(1):159-173.e9
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.2292.2021
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.
Mol Cell, 2022, S1097-2765(22)00394-X
EMBO Rep, 2022, e54801
Proc Natl Acad Sci U S A, 2022, 119(12):e2114336119
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
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.
Cell Rep, 2022, 38(5):110329
Front Immunol, 2022, 13:853894
Aging Dis, 2022, 13(1):313-328
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.
J Proteome Res, 2022, 21(4):1073-1082
bioRxiv, 2021, 10.1101/2021.03.17.435124
Commun Biol, 2021, 4(1):336
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.
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.
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.
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
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.
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, 2022, 29(4):545-558.e13
Adv Sci (Weinh), 2022, e2104299
Nat Commun, 2022, 13(1):2387
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.
Nat Commun, 2022, 13(1):3034
J Cell Biol, 2022, 221(1)e202103033
Adv Sci (Weinh), 2021, e2004846
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 Metab, 2022, S1550-4131(21)00542-8
Sci Rep, 2022, 12(1):7
EMBO Rep, 2021, e51503
S9850New (E/Z)-GO289

(E/Z)-GO289 potently and selectively inhibits casein kinase 2 (CK2) at an IC50 of 7 nM in vitro kinase assay.

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.

E2826New 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.
S9850New (E/Z)-GO289

(E/Z)-GO289 potently and selectively inhibits casein kinase 2 (CK2) at an IC50 of 7 nM in vitro kinase assay.

Tags: Casein Kinase inhibitor|Casein Kinase agonist|Casein Kinase activator|Casein Kinase inducer|Casein Kinase antagonist|Casein Kinase signaling pathway|Casein Kinase assay kit