ck2-in-1

CK2 inhibitor

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.

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.

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.

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.

Yck2-IN-1 (Compound 2a) is an inhibitor of the fungus Candida albicans Yck2. It has an IC50 of approximately 80 nM for Yck2 and an MIC80 of 12.5 µM for C. albicans, demonstrating good metabolic stability [66% remaining in mouse liver microsomes]. In a mouse model with drug-resistant Candida, Yck2-IN-1 significantly reduced fungal load in the kidneys. Yck2-IN-1 shows potential for research in antifungal infection treatments.

CK2-IN-12 (Compound 39) is an inhibitor of protein kinase CK2 with an IC50 of 0.8 μM.

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.

ROCK2-IN-11 (Compound A20) is a selective ROCK2 inhibitor with an IC50 of 0.18 μM against ROCK2, demonstrating greater potency over ROCK1. It is applicable in the research of idiopathic pulmonary fibrosis and chronic graft-versus-host disease (cGVHD).

ROCK2-IN-12 (Compound A25) is a selective inhibitor of ROCK2, exhibiting an IC50 of 7.0 nM for ROCK2, demonstrating greater efficacy compared to ROCK1 inhibition. It exerts potent anti-fibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. In a Bleomycin-induced mouse pulmonary fibrosis (PF) model, ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrosis progression. This compound is applicable in research on pulmonary diseases such as lung fibrosis.

ROCK2-IN-13 is a selective inhibitor of ROCK2. It functions by hindering ROCK2 kinase activity and reducing its nuclear expression, consequently disrupting the interaction between ROCK2 and transcription co-activators p300 and PGC 1α, thereby suppressing oncogene transcription. ROCK2-IN-13 activates FOXO1-driven PTEN expression, which in turn inhibits the PI3K/Akt pathway, induces G2/M cell cycle arrest, and promotes apoptosis (apoptosis). This compound effectively eliminates the nuclear transcription function of ROCK2 that maintains oncogenic signaling and restores the tumor-suppressive PTEN/FOXO1 axis. ROCK2-IN-13 is utilized in prostate cancer research.

DOCK2-IN-1 is a selective DOCK2 inhibitor (IC50 = 0.51 μM). It suppresses lymphocyte migration and cytoskeleton reorganization by blocking DOCK2-mediated Rac activation, used for immune response and transplant rejection research.

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.

CK2-IN-10 (31) is an allosteric inhibitor of CK2, applicable in cancer research.

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/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 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].