ck2 inhibitor 2

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 inhibitor4 (compound 5b) is a protein kinase CK2 inhibitor with an IC50 of 3.8 μM. It is applicable in tumor research.

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].

UCK2 Inhibitor-2 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2) with IC50=3.8 µM that inhibits UCK2-mediated nucleoside recycling in cells.

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).

(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.

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).

PIM-1/CK2-IN-2 (compound 3aA) is an inhibitor of the PIM-1/CK2 enzymes. This compound can induce the mitochondrial apoptosis pathway in CCRF-CEM cells and is utilized in cancer research.

Antiproliferative agent-46 is an inhibitor of the casein kinase 2 enzyme (CK2) receptor and exhibits potent antiproliferative activity, with an IC50 value of 5.75 μM against the U87 cell line.

CK2-IN-15 (Compound Biv5) is a selective and potent inhibitor of the enzyme protein kinase CK2, with an IC50 value of 51 pM. It significantly reduces the replication of SARS-CoV-2 in HEK-ACE2-TMPRSS2 and Vero cells, and also decreases viral replication in an in vitro model of human nasal epithelial cells. CK2-IN-15 holds potential for research into diseases related to β-coronavirus infections.

IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDAC. It exhibits high selectivity for CK2 with an IC50 of 1.7 nM and demonstrates broad inhibitory activity against HDAC (HDAC1, 2, 3, and 6) with IC50 values of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, while showing low activity against HDAC8. IOR-160 modulates critical cell signaling pathways by inhibiting AKT phosphorylation and increasing α-tubulin acetylation. The compound reduces tumor growth and burden through its dual inhibition of CK2/HDAC and is relevant for research on triple-negative breast cancer.

BMS-135 is a potent and selective ATP-competitive inhibitor of casein kinase 2 (CK2), with IC50 values of 0.8 nM for CK2α and 0.3 nM for CK2α' isoforms. It mimics the structure of ATP, binding to the active site of CK2 and inhibiting its serine/threonine phosphorylating activity. BMS-135 effectively inhibits cell proliferation and demonstrates antitumor properties, making it useful for research in colon cancer.

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

IQA is a casein kinase 2 (CK2) inhibitor.

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

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].

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.

CK2-IN-7 (compound 2), a casein kinase 2 (CK2) inhibitor, demonstrates a synergistic effect when used in combination with a structurally distinct CK2 chemical probe, SGC-CK2-1, in targeting cancer [1].

CIGB-300 acetate (P15-Tat acetate) is a peptide that acts as an inhibitor of casein kinase 2 (CK2). It exhibits anticancer properties by disrupting the phosphorylation activity of CK2. CIGB-300 acetate induces apoptosis in various tumor cell lines and is applicable for cancer research.