Catalog No.
Product Name
Application
Product Information
Citations
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Casein Kinase Inhibitor
4,5,6,7-Tetrabromo-1H-benzimidazole is a selective inhibitor of casein kinase 2 (CK2), functioning through an ATP-competitive mechanism. This compound has been shown to effectively inhibit CK2 activity, making it a valuable tool for investigating the role of CK2 in various cellular processes. Its primary applications include studies on cell proliferation, apoptosis, and signal transduction pathways. Researchers may utilize this reagent to explore CK2's involvement in cancer and other disease states. -
CK1 Inhibitor
CK1δ-IN-7 is a selective inhibitor of casein kinase 1δ (CK1δ), a crucial mediator in various cellular signaling pathways. This compound exhibits potent inhibition of CK1δ activity, making it a valuable tool for investigating the role of CK1δ in cellular processes such as circadian rhythms, cellular proliferation, and apoptosis. Researchers can utilize CK1δ-IN-7 in studies related to cancer, neurodegenerative diseases, and other pathophysiological conditions linked to CK1δ signaling dysregulation. -
CK1δ Inhibitor
CK1δ-IN-8 is a selective inhibitor of casein kinase 1 delta (CK1δ), a crucial regulator in various cellular signaling pathways. This compound demonstrates significant potential in Alzheimer's disease research by modulating phosphorylation processes linked to protein aggregation and neurodegeneration. Its application may aid in elucidating the molecular mechanisms underlying Alzheimer's and developing therapeutic strategies. -
CK1δ Inhibitor
Casein kinase 1δ-IN-30 is a selective inhibitor of Casein kinase 1δ (CK1δ). This compound demonstrates significant biological activity in modulating CK1δ activity, making it a valuable tool for investigating neurodegenerative diseases and related pathways. Its application in research can enhance understanding of CK1δ's role in cellular processes and potential therapeutic targets in neurodegeneration. -
CK1δ Inhibitor
CK1δ-IN-5 is a selective inhibitor of Casein kinase 1δ (CK1δ), a key enzyme involved in various cellular processes. This compound plays a significant role in the study of neurodegenerative diseases by modulating upstream signaling pathways that may contribute to neuronal dysfunction. Researchers can utilize CK1δ-IN-5 to explore potential therapeutic targets and elucidate the molecular mechanisms underlying these diseases. -
CK1 Inhibitor
CK1-IN-5 is a selective inhibitor of Casein Kinase 1 (CK1). It has been shown to extend the circadian period by inhibiting the activity of AtCKL3 and AtCKL4. This compound is of significant interest in circadian rhythm research and offers potential applications in studies of sleep disorders and metabolic regulation. -
CK1δ/1ε Inhibitor
SR-2890 is a highly selective ATP-competitive inhibitor of casein kinase 1 delta (CK1δ) and 1 epsilon (CK1ε), exhibiting IC50 values of 4 nM and 44 nM, respectively. This compound effectively inhibits the serine/threonine kinase activity of CK1δ and has demonstrated antiproliferative effects against human A375 melanoma cells. Additionally, SR-2890 has shown potential utility in research related to melanoma and in studying diseases associated with CK1δ/ε, such as Alzheimer's disease, due to its favorable in vivo pharmacokinetic properties and metabolic stability. -
Pro-Apoptotic Peptide
CIGB-300 is a pro-apoptotic peptide that targets casein kinase 2 (CK2). It exhibits potent anticancer activity by disrupting CK2 phosphorylation, leading to apoptosis in various tumor cell lines. This compound is valuable for cancer research, particularly in studies focused on apoptosis and CK2 modulation. -
p38/CK1 Inhibitor
Casein kinase 1δ-IN-29 is a potent inhibitor of p38α and casein kinase 1, demonstrating IC50 values of 0.041 µM for p38α, 0.005 µM for CK1δ, and 0.447 µM for CK1ε. This compound effectively interrupts the cell cycle at the subG1 phase and induces apoptosis in AC1-M88 cells. It serves as a valuable tool in research applications focused on cell cycle regulation and apoptosis pathways. -
Hsp90-Cdc37 PPI Inhibitor
Hsp90-Cdc37-IN-4 is a selective inhibitor of the Hsp90-Cdc37 protein-protein interaction (PPI). This compound disrupts the interaction by inhibiting casein kinase 2 (CK2), leading to reduced phosphorylation of Cdc37 at Serine 13. In cellular assays, Hsp90-Cdc37-IN-4 has been shown to induce G0/G1 cell cycle arrest and activate apoptotic pathways via the mitochondria. Additionally, it exhibits significant anti-breast cancer properties, making it a valuable tool in cancer research. -
CK1α Inhibitor
Casein Kinase Inhibitor A86 is a selective inhibitor of casein kinase 1α (CK1α), demonstrating potent oral bioactivity. In addition to its primary target, A86 also inhibits cyclin-dependent kinase 7 (CDK7) and cyclin-dependent kinase 9 (CDK9), contributing to its diverse pharmacological profile. This compound has been shown to induce apoptosis in leukemia cells, highlighting its potential as an anti-leukemic agent in cancer research applications. -
CK1ε Inhibitor
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. -
Casein Kinase/DYRK/TNIK Inhibitor
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. - Ellagic acid is a natural phenol antioxidant found in numerous fruits and vegetables. The antiproliferative and antioxidant properties of ellagic acid have spurred preliminary research into the potential health benefits of ellagic acid consumption.
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CK1 inhibitor
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). -
ATP-competitive CK2 inhibitor
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. - Casein Kinase 2 Substrate Peptide is a common CK2 substrate peptide. Casein Kinase 2 Substrate Peptide is synthesized with its C-terminus conjugated to 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid (EDANS). Casein Kinase 2 Substrate Peptide can be used for protein kinase CK2 activity determination.
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CK2 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. -
CK2 Inhibitor
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. -
CDK Inhibitor
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. -
CK1α Molecular Glue
BMS-986397 is a selective and orally active cereblon-based molecular glue degrader targeting casein kinase 1α (CK1α). This compound effectively induces apoptosis and cell cycle arrest in acute myeloid leukemia (AML) cells, positioning it as a valuable tool for research in the fields of AML and high-risk myelodysplastic syndromes (HR-MDS). Its unique mechanism offers potential for elucidating CK1α's role in these malignancies. -
BRD4/CK2 inhibitor
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. -
CK2/ERK8 inhibitor
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. -
CK1α degrader
TMX-4116 is a selective degrader of casein kinase 1α (CK1α), demonstrating preferential degradation activity with DC₅₀ values below 200 nM in MOLT4, Jurkat, and MM.1S cell lines. By targeting CK1α for proteasomal degradation, TMX-4116 offers a promising tool for investigating CK1α function and holds potential for therapeutic research in multiple myeloma and related hematologic malignancies. -
CK1α molecular glue degrader
SJ3149 is a selective and potent molecular glue degrader that targets casein kinase 1α (CK1α) for proteasomal degradation. By promoting CK1α elimination, SJ3149 exhibits broad antiproliferative activity across various cancer models. It serves as a valuable tool for exploring CK1α-dependent signaling pathways and holds promise for therapeutic development in oncology research. -
TAK1 inhibitor
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). -
CK2 chemical probe
SGC-CK2-1 is a highly potent, ATP-competitive, and cell-permeable chemical probe that selectively targets casein kinase 2 (CK2), exhibiting IC₅₀ values of 36 nM for CK2α and 16 nM for CK2α′ in the nanoBRET assay. With exclusive selectivity for both human CK2 isoforms, SGC-CK2-1 serves as a valuable tool for studying CK2-related signaling pathways and holds potential for research in neurodegenerative diseases. -
CK1α activator
SSTC3 is a potent activator of casein kinase 1α (CK1α), with a binding affinity (K_d) of 32 nM, and functions as an inhibitor of WNT/β-catenin signaling with an EC₅₀ of 30 nM. Unlike many conventional WNT pathway inhibitors, SSTC3 demonstrates minimal gastrointestinal toxicity, offering a promising therapeutic strategy for targeting WNT-driven cancers with improved safety profiles. -
Casein Kinase inhibitor
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. -
PDE6D/IKZF1/IKZF3/CK1α Degrader
FPFT-2216 is a “molecular glue” degrader that facilitates the proteasomal degradation of multiple target proteins, including phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3), as well as casein kinase 1α (CK1α). By promoting selective ubiquitination through E3 ligase recruitment, FPFT-2216 modulates key regulatory pathways and holds promise for research in oncology and inflammatory diseases. -
Casein Kinase Inhibitor
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 Inhibitor
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. -
CK2/HDAC Inhibitor
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. -
CK2 Inhibitor
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. -
Molecular Glue Degrader
WEE1 Degrader 1 is a CRBN-dependent molecular glue degrader that targets WEE1 and casein kinase 1α (CK1α) with sub-2 nM DC50 values for both proteins. This compound effectively induces the proteasomal degradation of its targets, providing a valuable tool for studying cell cycle regulation. WEE1 Degrader 1 is particularly relevant in the research of acute lymphoblastic leukemia, acute monocytic leukemia, acute promyelocytic leukemia, colorectal adenocarcinoma, and diffuse large B-cell lymphoma. -
PKC Substrate
Myelin Basic Protein (MHP4-14) serves as a specific substrate for protein kinase C (PKC), demonstrating a Km of 7 μM. This synthetic peptide, derived from residues 4-14 of myelin basic protein, is not phosphorylated by various other kinases, including cyclic AMP-dependent protein kinase and casein kinases I and II. It is highly effective for studying PKC activity in crude tissue extracts, providing a low background and reliable results in biochemical assays.
