ck2-in-1

CK2 inhibitor

BRD4 CK2-IN-1 is a small molecule inhibitor targeting BRD4 and CK2, with an IC50 of 180nM for BRD4 and 230nM for CK2. It inhibits the proliferation of MDA-MB-231 and MDA-MB-468 cells, inducing apoptosis and autophagy-related cell death. It can be used in triple-negative breast cancer research.

HDAC CK2-IN-1 (compound 38) acts as an inhibitor of HDAC1 (IC 50 = 1.46 μM), HDAC6 (IC 50 = 0.66 μM), and CK2 (IC 50 = 3.67 μM). It demonstrates promising antiproliferative effects on various cell lines, including Jurkat, MCF-7, HCT-116, and HL-60.

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).

ROCK2-IN-10 is an effective ROCK inhibitor, which is widely used in the research fields of cell migration, invasion, differentiation, proliferation, immune response, drug resistance, cytoskeletal dynamics, etc.

CK2 PIM1-IN-1 is an inhibitor of CK2 (IC50: 3.787 μM) and PIM1 (IC50: 4.327 μM), developed for researching proliferative disorders like cancer and other kinase-associated conditions.

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.

CK2-IN-14 (Compound 10b) is an inhibitor of cyclin-dependent kinase 2α with an IC50 of 36.7 nM. It effectively hinders the growth of cancer cell lines 786-O and U937, with GI50 values of 7.3 μM and 7.5 μM, respectively.

CK2-IN-13 (compound 12c) is a potent inhibitor of CK2, with an IC50 value of 5.8 nM, playing a significant role in cancer research.

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].

CK2-IN-11 (32) acts as an allosteric inhibitor of CK2, with IC50 values of 19.3 nM for the CK2α2β2 isoform and 15.6 nM for the CK2α'2β2 isoform.

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 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].

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-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].

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