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].

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

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).

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

(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.

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

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].