Casein Kinase

Orobol is a selective inhibitor of Casein Kinase 1 epsilon (CK1ε) with demonstrated anti-skin-aging and anti-obesity effects. It targets multiple kinases, including VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK, exhibiting inhibitory activity with IC50 values ranging from 1.24 to 4.45 μM. Additionally, Orobol inhibits various phosphoinositide 3-kinase (PI3K) isoforms, specifically showing activity with IC50 values between 3.46 and 5.27 μM for PI3K α/β/γ/K/δ. These properties make Orobol valuable for investigating signaling pathways related to cellular growth, metabolism, and aging.

ON 108600 is a potent inhibitor of casein kinase 2 (CK2), TYRK1 (DYRK), and TNIK, demonstrating IC50 values of 0.016 μM against DYRK1A, 0.007 μM against DYRK2, 0.05 μM against CK2α1, 0.005 μM against CK2α2, and 0.005 μM against TNIK. This compound exhibits promising antitumor activity, making it a valuable tool for research applications focused on cancer biology, signaling pathways, and kinase inhibition studies. Its specificity for these kinases positions ON 108600 as a critical reagent for investigating therapeutic strategies targeting kinase-related diseases.

Epiblastin A is an inhibitor of Casein Kinase 1 (CK1) that engages CK1 isoenzymes in cell lysate and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs).

Ellagic acid hydrate is a natural antioxidant, and acts as a potent and ATP-competitive CK2 inhibitor, with an IC50 of 40 nM and a Ki of 20 nM.

BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC50 of ~4 nM. BioE-1115 is also a potent casein kinase 2α inhibitor with an IC50 of ~10 μM.

CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM.CKI-7 is a selective Cdc7 kinase inhibitor.

CK2-TN03 is an ATP-competitive inhibitor of casein kinase 2 (CK2), demonstrating an IC50 of 165 nM and a Ki of 20 nM. This compound effectively inhibits CK2-mediated activation of survivin and reduces phosphorylation levels of critical proteins such as BRD4/MYCN and AKT1. CK2-TN03 has shown significant anti-neuroblastoma effects by promoting mitotic catastrophe and apoptosis in cancer cells, making it a valuable tool for research focused on neuroblastoma.

CX-5011 free base is a potent inhibitor of casein kinase 2 (CK2), targeting this serine/threonine kinase to modulate cellular signaling pathways. It also serves as a Rac-1 activator, enhancing processes such as methuosis and macropinocytosis. The compound has been shown to induce apoptosis and decrease the phosphorylation of ribosomal protein S6 (rpS6), making it a valuable tool for research applications in cancer biology and cellular metabolism.

5,6-Dichlorobenzimidazole riboside (DRB) functions as a selective inhibitor of several carboxyl-terminal domain kinases, notably casein kinase II and cell cycle-dependent kinases (CDKs). This nucleoside analog exhibits antitumor activity and has been shown to induce apoptosis in targeted cancer cells. Its role in modulating kinase activity makes DRB valuable for research in cancer biology and cell cycle regulation.

BRD4/CK2-IN-1 is the first highly potent and orally active dual inhibitor of BRD4 and casein kinase 2 (CK2), with IC₅₀ values of 180 nM and 230 nM, respectively. It exhibits strong anticancer activity with minimal toxicity, and induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC) cells.

TMCB (CK2/ERK8-IN-1) is a dual inhibitor of casein kinase 2 (CK2) and ERK8 (MAPK15/ERK7), with a Ki of 0.25 µM for CK2 and IC50 values of 0.50 µM for both targets. It also exhibits binding affinity for PIM1 (Ki = 8.65 µM), HIPK2 (Ki = 15.25 µM), and DYRK1A (Ki = 11.9 µM). CK2/ERK8-IN-1 demonstrates pro-apoptotic activity and is a useful tool for studying kinase-mediated cell survival pathways.

HS-276 is an orally bioavailable, potent, and highly selective inhibitor of transforming growth factor-β–activated kinase 1 (TAK1), with a Kᵢ of 2.5 nM. It exhibits strong inhibition of TAK1 and moderate activity against a panel of other kinases, including CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with respective IC₅₀ values ranging from 8.25 to 5585 nM. HS-276 is a valuable tool for investigating TAK1-mediated signaling pathways and holds therapeutic potential for inflammatory conditions such as rheumatoid arthritis (RA).

BTX-A51 (Casein Kinase Inhibitor A51) is a potent, orally bioavailable inhibitor of casein kinase 1α (CK1α). It effectively induces apoptosis in leukemia cells and demonstrates strong anti-leukemic activity in preclinical models, making it a promising therapeutic candidate for hematologic malignancies.

Hematein is an allosteric inhibitor of casein kinase II, exhibiting an IC50 of 0.74 μM. It demonstrates significant biological activity by inhibiting Akt/PKB Ser129 phosphorylation and the Wnt/TCF signaling pathway. Research applications include studying apoptosis in lung cancer cells, making it a valuable reagent for cancer biology investigations.

HDAC/CK2-IN-1 is an inhibitor targeting histone deacetylases HDAC1 and HDAC6, with IC50 values of 1.46 μM and 0.66 μM, respectively, as well as casein kinase 2 (CK2) with an IC50 of 3.67 μM. This compound demonstrates significant antiproliferative effects on various cancer cell lines, including Jurkat, MCF-7, HCT-116, and HL-60. It serves as an important research tool for studying the roles of histone modifications and CK2 in tumor biology and could have potential implications in the development of cancer therapeutics.

IOR-160 is a dual inhibitor targeting casein kinase 2 (CK2) and histone deacetylases (HDACs). It showcases high selectivity for CK2, with an IC50 of 1.7 nM, and demonstrates broad inhibitory effects on HDACs 1, 2, 3, and 6, with IC50 values of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively. Through the inhibition of AKT phosphorylation and the enhancement of acetylated α-tubulin levels, IOR-160 effectively modulates critical cellular signaling pathways. This compound is particularly relevant in research focused on triple-negative breast cancer, where it has been shown to inhibit tumor growth and reduce tumor burden.

CX-5011 is a selective inhibitor of casein kinase 2 (CK2), a serine/threonine kinase involved in cellular signaling pathways. This compound has been shown to activate Rac1, leading to effects on cell motility and morphology. Notably, CX-5011 induces apoptosis in various cancer cell lines, thereby promoting cancer cell death and making it a valuable tool for research in cancer biology and therapeutic interventions targeting CK2.