Casein Kinase

Inhibitory Selectivity

Isoform-specific Inhibitors

Casein Kinase Products

Catalog No. 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.

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.

S2805

LY364947

LY364947 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.

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.

S0707New

Silmitasertib sodium salt

Silmitasertib sodium salt is a potent, orally bioavailable and selective inhibitor of casein kinase 2 (CK2) with IC50 of 1 nM against CK2α and CK2α'.

S2249New

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).

S6734New

PF-670462

PF-670462 is a potent and selective inhibitor of CK1ε and CK1δ with IC50 value of 90 nM and 13 nM, respectively.

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.

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.

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.

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.

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.

S8237

IC261

IC261 is a novel inhibitor of CK1. The IC50 of IC261 for CK1 is 16 μM and for Cdk5 is 4.5 mM.

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.

Catalog No. 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.

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.

S2805

LY364947

LY364947 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.

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.

S0707New

Silmitasertib sodium salt

Silmitasertib sodium salt is a potent, orally bioavailable and selective inhibitor of casein kinase 2 (CK2) with IC50 of 1 nM against CK2α and CK2α'.

S2249New

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).

S6734New

PF-670462

PF-670462 is a potent and selective inhibitor of CK1ε and CK1δ with IC50 value of 90 nM and 13 nM, respectively.

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.

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.

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.

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.

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.

S8237

IC261

IC261 is a novel inhibitor of CK1. The IC50 of IC261 for CK1 is 16 μM and for Cdk5 is 4.5 mM.

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.