Casein Kinase

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

Silmitasertib (CX-4945) is a potent, orally bioavailable inhibitor of casein kinase 2 (CK2; Ki: 0.38 nM).

XL-413 is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. XL-413 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induct

PF-670462 is a potent (IC50 = 7.7 ± 2.2 nM) and selective (>30-fold with respect to 42 additional kinases) inhibitor of CK1ε in isolated enzyme preparations.

IWP-2 is a Wnt pathway inhibitor (IC50=27 nM) and an ATP-competitive CK1δ inhibitor (IC50=40 nM for M82FCK1δ). IWP-2 inhibits self-renewal of embryonic stem cells and has been used in stem cell and organoid research.

Ellagic acid (Gallogen), a thickened tetracyclic natural product, is a potent CK2 inhibitor (IC50=40 nM; Ki=20 nM) with ATP-competitive properties. Ellagic acid is an antioxidant and also possesses antiproliferative activity.

WAY-297174 is a human protein kinase CK2 inhibitor with IC50 of > 33 μM.

Emodin (Frangula emodin) is a naturally occurring anthraquinone present in the roots and barks of numerous plants; exerts antiproliferative effects in Y cells that are regulated by different signaling pathways.

TBCA (Casein Kinase II Inhibitor III, TBCA) is a highly selective CK2 (casein kinase II) inhibitor, IC50 = 110 nM, Ki = 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases.

Silmitasertib sodium salt (CX-4945 sodium salt) is a potent and orally bioavailable, highly selective inhibitor of CK2(IC50 of 1 nM, CK2α).

XL413 hydrochloride (BMS-863233 Hydrochloride) is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC 50 of 3.4 nM. XL413 hydrochloride also exhibits potent effect with IC 50 s of 215, 42 nM on CK2, PIM1, respectively, and an EC 50 of 118 nM on pMCM.

AS-252424 is a potent and selective inhibitor of PI3Kγ with an IC50 of 33 nM and demonstrates over 10-fold selectivity for PI3Kγ versus PI3Kα.

Casein Kinase inhibitor A51 is an orally active casein kinase 1α (CK1α) inhibitor with anticancer activity that induces apoptosis in leukemia cells, and may be used in the study of neck cancers, acute myeloid leukemia, breast and prostate cancers.

SSTC3 is a casein kinase 1α (CK1α) activator and a potent HIF1α inhibitor, each with a Kd of 32 nM. It has potential antitumor activity, inhibits WNT signaling, and suppresses SHH medulloblastoma tumor growth.

NMS-P715 is a selective and ATP-competitive MPS1 inhibitor(IC50 of 182 nM).

SGC-CK2-1 is a highly specific inhibitor of CK2, a inducer of insulin production and secretion in pancreatic β-cells, and can be used in the study of neurodegenerative diseases.

LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.

Casein kinase 1δ-IN-6 is a potent and selective inhibitor of the protein kinase CK-1δ with an IC50 of 23 nM, demonstrating neuroprotective and anti-inflammatory activity in both in vitro and in vivo assays. Casein kinase 1δ-IN-6 can be used to study neurodegenerative diseases.

CK2 Inhibitor 2, characterized as a potent, selective, and orally active inhibitor of CK2, demonstrates an impressive IC50 value of 0.66 nM. It exhibits high selectivity towards Clk2 with an IC50 of 32.69 nM in comparison to CK2. Furthermore, CK2 Inhibitor 2 has been shown to possess promising antiproliferative and antitumor activities [1].

SR-3029 is a highly potent and specific inhibitor of CK1δ CK1ε.

A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).

FPFT-2216 is a molecular gel that degrades IKZF6, IKZF1, DE1D, and CK3α.FPFT-2216 has potential antitumor activity and can be used to study diseases of the immune system.FPFT-2216 is a molecular gel that degrades IKZF6, IKZF1, DE1D, and CK3α.

MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM.

TAK-715 is a p38 MAPK inhibitor for p38α.

D4476 (Casein Kinase I Inhibitor) is an effective, selective, and cell-permeant CK1 (casein kinase 1) inhibitor( IC50=300 nM in a cell-free assay).

PF-4800567 is a selective inhibitor of casein kinase 1ε (CK1ε; IC50 = 32 nM) with greater than 20-fold selectivity over CK1δ.

XL413 HCl is an ATP-competitive Cdc7 inhibitor (IC50: 3.4 nM) that is potent and selective.XL413 HCl inhibited CK2 and PIM1 with IC50 values of 215 and 42 nM, respectively.XL413 HCl showed an EC50 value of 118 against pMCM.

DMAT (Casein kinase II Inhibitor) is a potent and specific inhibitor of CK2(IC50 value of 130 nM).

LH846 is a selective inhibitor of CK1δ with IC50 values of 290 nM for CK1δ, 1.3 μM for CK1ε, and 2.5 μM for CK1α, and exhibits no inhibitory activity at CK2.

TBB (NSC-231634)(NSC-231634) is a highly selective, ATP GTP-competitive inhibitor of casein kinase-2 (CK2).

CK2α-IN-1 is a selective non-ATP-competitive CK2α inhibitor with an IC50 of 7.0 µM and a Ki of 1.6 µM.CK2α-IN-1 exhibits potential anticancer activity and can be used in cancer research.

CK1-IN-1 (PUN51207) is a casein kinase 1 (CK1) inhibitor. CK1-IN-1 has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively.

Casein kinase 1δ-IN-3 (Compound 23a) is an inhibitor of casein kinase 1 delta (CK1δ) with a pIC50 of 6.5376 M.

Epiblastin A is an inhibitor of Casein Kinase 1 (CK1). Epiblastin A engages CK1 isoenzymes in cell lysate and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs).

BioE-1115 is a selective and potent inhibitor of serine-threonine protein kinase (PASK, IC50 = 4 nM). BioE-1115 is a potent inhibitor of CK2α (IC50 = 10 μM).

IC261 (SU-5607) is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It inhibits PKC and casein kinase I with Ki values of 47 μM and 80 μM, respectively[1], and also inhibits PKA (Ki=4.3 μM), casein kinase II (Ki=5.1 μM), and myosin light chain kinase (MLCK) (Ki=7.4 μM).

Casein kinase 1δ-IN-7 is a Casein kinase 1δ inhibitor for neurodegenerative diseases such as Alzheimer's disease.

CKI-7 is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. It also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

CK2/ERK8-IN-1 (TMCB) is a dual inhibitor of casein kinase 2 (CK2) (Ki: 0.25 µM) and ERK8 (IC50s: 0.50 μM) with pro-apoptotic efficacy. CK2/ERK8-IN-1 also binds to PIM1, DYRK1A, and HIPK2 (Kis: 8.65 µM, 11.9 µM, and 15.25 µM).

CK2-IN-4 is a protein kinase (CK2) inhibitor with an IC50 value of 8.6 µM. CK2-IN-4 has potential anticancer ah and anti-inflammatory activity for the study of viral infections and glomerulonephritis diseases.

Casein Kinase II Inhibitor IV is an inducer of epidermal keratinocyte differentiation.

CK1-IN-3 is casein kinase 1 (CK1) inhibitor and can be used for research on the treatment or prevention of diseases associated with circadiantiazol rhythm, inflammation diseases.

TA-01 is a potent inhibitor of CK1 and p38 MAPK, with IC50 values of 6.4 nM for CK1ε, 6.8 nM for CK1δ, and 6.7 nM for p38 MAPK.

NCC007 is a novel CKIα and CKIδ dual inhibitors by structural modification of N9 and C2 position of longdaysin.

Longdaysin is an inhibitor of CK1α and CK1δ (IC50s: 5.6 8.8 µM). It also can inhibit ERK2 (IC50: 52 µM).

(E/Z)-GO289, which strongly lengthened circadian period, is a potent and selective inhibitor of CK2. (E/Z)-GO289 exhibited cell type-dependent inhibition of cancer cell growth that correlated with cellular clock function. The discovery of (E/Z)-GO289 provides a direct link between the circadian clock and cancer regulation and reveals unique design principles underlying kinase selectivity.

Ac-ESMD-CHO functions as an inhibitor of both caspase-3 and caspase-7, specifically obstructing the proteolytic cleavage of the caspase-3 precursor peptide (CPP32) at the Glu-Ser-Met-Asp (ESMD) site [1] [2].

Casein kinase 1δ-IN-4 (compound 567) is a potent inhibitor of casein kinase 1δ with potential application in Alzheimer's disease research [1].

CK1-IN-2 (compound Nr.4) is a potent inhibitor of CK1, with IC50 values of 123 nM for CK1a, 19.8 nM for CK1d, 26.8 nM for CK1e, and 74.3 nM for p38a [1].