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.

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.

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).

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.

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.

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

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.

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

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

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

TAK-715 is a p38 MAPK inhibitor for p38α.

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

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

Ellagic acid (Gallogen) is a fused four ring compound isolated from the kino of Eucalyptus maculata Hook and E. Hemipholia F. Muell. Activates Factor XII of the blood clotting system which also causes kinin release; used in research and as a dye.

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

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.

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

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.

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

Ellagic acid (hydrate) is a natural antioxidant and acts as a potent and ATP-competitive CK2 inhibitor (IC50:40 nM, Ki: 20 nM).

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

Casein kinase 1δ-IN-8 is an inhibitor of casein kinase 1δ and is used to treat neurodegenerative diseases such as Alzheimer's disease type.

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-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.

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

PF-5006739 is an effective and selective inhibitor of CK1δ/ε (IC50s: 3.9 nM and 17.0 nM, respectively). PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selecti

TTP 22 is a high affinity, ATP-competitive casein kinase 2 (CK2) inhibitor with IC50/Ki of 0.1 uM/40 nM, and shows selectivity >250-fold for CK2 over JNK3, ROCK1, and MET(IC50> 10 uM).

LH846 is a selective inhibitor of CK1δ (IC50 values are 290 nM, 1.3 uM and 2.5 uM for CK1δ, ε and α); exhibits no inhibitory activity at CK2.

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

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

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).

TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC50s of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively.

IWP-2, an inhibitor of Wnt processing and secretion (IC50=27 nM) in a cell-free assay, selectively blocks Porcn-mediated Wnt palmitoylation.

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.

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.

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively[1]. A-3 hydrochloride against P

Casein kinase 1δ-IN-10 is an inhibitor of casein kinase 1δ (CK1δ).

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

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

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).

CX-5011, a CK2 inhibitor, induces Rac1 activation and promotes apoptosis, effectively causing cancer cell death [1] [2].

Casein kinase 1δ-IN-6 is a potent and selective inhibitor of the protein kinase CK-1δ with an IC50 of 23 nM.Casein kinase 1δ-IN-6 shows 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.

PI-828 is a phosphatidylinositol 3-kinase (PI3K) inhibitor, which is widely used to study the physiological function of PI3K and also promotes stem cell differentiation into mesoderm.

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].

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.

ON 108600 is a chemical inhibitor targeting CK2 (Casein Kinase 2), TNIK, and DYRK1, demonstrating IC50 values of 0.016 μM and 0.007 μM for DYRK1A and DYRK1B, 0.028 μM for DYRK2, 0.05 μM and 0.005 μM for CK2α1 and CK2α2, and 0.005 μM for TNIK, respectively. This compound exhibits antitumor activity [1].

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

(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.

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.