ck2

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].

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.

CK2 inhibitor

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.

CK2-IN-9, a potent and selective CK2 kinase inhibitor, exhibits an inhibitory concentration (IC50) of 3 nM against its target enzyme and hampers Wnt reporter activity with an IC50 of 75 nM. In rats, it demonstrates low exposure (AUC=0.36 μM/h) and high clearance (CL=65 mL/min/kg) [1].

BRD4/CK2-IN-1 is the first potent, orally active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), acting on both BRD4 (IC50: 180 nM) and CK2 (IC50: 230 nM). In triple-negative breast cancer (TNBC), BRD4/CK2-IN-1 induces apoptosis and autophagy-related cell death.

CK2-IN-3 is a potent and selective CK2 inhibitor (Kd: 12 nM) with IC50 values of 1.51 μM for CK2α and 7.64 μM for CK2α'. CK2-IN-3 can be used in cancer research.

CK2-IN-6, a powerful inhibitor of protein kinase CK2, shows promise for research in cancer, along with conditions related to kinases such as inflammation, pain, and specific immune diseases.

CK2 inhibitor 3 is a highly potent inhibitor of protein kinase CK2, exhibiting an IC50 value of 280 nM. It effectively inhibits the intracellular activity of CK2 and displays a notable impact on the viability of tumor cells. Moreover, CK2 inhibitor 3 demonstrates exceptional selectivity among a diverse panel of 320 kinases [1].

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.

CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1 (IC50s: 3.787 μM and 4.327 μM). It is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions.

Benzenamine, 2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)- is a useful organic compound for research related to life sciences. The catalog number is T9797 and the CAS number is 1072906-07-0.

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

CK-2-68 is a potent inhibitor of PfNDH2.

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.

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.

ROCK2-IN-2 is a selective inhibitor of ROCK2 (IC50 of <1 μM).

ROCK2 inhibitor is a chemical compound associated with the therapeutic management of psoriasis. It exhibits its efficacy in targeting ROCK2 enzymes within HaCaT cells and has demonstrated beneficial effects in a psoriasis-like mouse model.

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

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

ROCK2-IN-6 (Comp A) is a selective inhibitor of ROCK2, applicable in the study and treatment of ROCK-mediated, autoimmune, and inflammatory diseases [1].

ROCK2-IN-5, a compound integrating structural elements from the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids, exhibits a favorable multitarget profile and tolerability. It shows potential for research in Amyotrophic Lateral Sclerosis (ALS) associated with a SOD1 mutation.

WNK-IN-B is an inhibitor of Wnk signalling. WNK-IN-B is a cell-permeable diaminoacridine derivative that targets the CCT domain of SPAK and OSR1 via reversible binding. WNK-IN-B selectively suppress hypotonic shock-induced WNK signaling pathway activation

UCK2 Inhibitor-3 is a non-competitive inhibitor targeting uridine-cytidine kinase 2 (UCK2), a key enzyme in the pyrimidine salvage pathway, with an IC50 value of 16.6 μM. Notably, UCK2 can partially substitute for dihydroorotate dehydrogenase (DHODH) in infected or rapidly dividing cells, facilitating effective uridine salvage. Furthermore, UCK2 Inhibitor-3 exhibits inhibition of DNA polymerase eta and kappa, with IC50 values of 56 μM and 16 μM, respectively.

UCK2 Inhibitor-1 is a non-competitive UCK2 inhibitor with an IC 50 of 4.7 µM .

UCK2 Inhibitor-2, a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2), exhibits an IC50 of 3.8 µM and effectively suppresses uridine salvage within cells.

ROCK2-IN-6 hydrochloride (Comp A) serves as a selective inhibitor of ROCK2, applicable for research into ROCK-mediated diseases, autoimmune disorders, and inflammation [1].

DOCK2-IN-1, an analogue of CPYPP, effectively inhibits DOCK2 (IC50 = 19.1 μM) by reversibly binding to its DHR-2 domain, thereby hindering its catalytic function. This compound obstructs the activation of Rac in lymphocytes, triggered either by chemokine or antigen receptors. Consequently, DOCK2-IN-1 markedly reduces chemotactic responses and T cell activation [1].

CCK2R Ligand-Linker Conjugate 1 is a hydrophilic peptide linker that conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) as ligand-linker conjugates[1].

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

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

Rottlerin (NSC-56346) is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.

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.

Casein Kinase 2 Substrate Peptide, a widely recognized CK2 substrate, is synthesized with its C-terminus conjugated to 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid (EDANS). This peptide serves as a tool for determining protein kinase CK2 activity [1].

QLT0267 is an inhibitor targeting integrin-linked kinase (ILK; IC50= 26 nM), showing over 10-fold selectivity against cyclin-dependent kinases 1, 2, and 5 (Cdk1, Cdk2, and Cdk5), and over 1,000-fold selectivity against C-terminal Src kinase (CSK), DNA-PK, Pim-1, Akt, PKC, and casein kinase 2 (CK2) at a concentration of 10 mg/ml. This compound effectively inhibits the proliferation of NPA187 papillary thyroid cancer cells with an IC50 of approximately 3 µM and induces apoptosis in NPA187, DRO, and K4 cancer cell lines. In vivo studies reveal that QLT0267, administered at 100 mg/kg, significantly reduces tumor growth in a DRO mouse xenograft model and diminishes both tumor volume and intratumoral vascularization in a U87MG glioblastoma mouse xenograft model, showcasing its potential for therapeutic applications in cancer treatment.

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

TID43, a CK2 inhibitor, exhibits potent inhibition with an IC50 value of 0.3 μM. It is applicable in anti-angiogenic research [1].

4,5,6,7-Tetrabromobenzimidazole is a selective and ATP-competitive inhibitor of protein kinase CK2 [1].

CK2 and ERK8 inhibitor

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).

Casein Kinase II Substrate, a peptide substrate, is selectively phosphorylated by casein kinase II (CK2) [1].

SRPIN-803 is a selective dual SRPK1 and CK2 inhibitor.

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).

CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.

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.

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

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].