Catalog No.
Product Name
Application
Product Information
Citations
- 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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Emodin is a purgative resin, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica). It belongs to a family of compounds called anthraquinones, which have shown anti-inflammatory and anticancer effects
- Roberto Brenes, .et al. , J Wildl Dis, 2022, Apr 1;58(2):341-347 PMID: 35255143
- Sakanashi M, .et al. , Circ J. , 2013, 77(7):1827-37. PMID: 23615023
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PI3K Inhibitor
LY294002 is a PI3k inhibitor (cell IC50 about 10 μM) and a casein kinase II inhibitor.- Yinhua Ni, .et al. , J Agric Food Chem, 2024, Jul 31;72(30):16708-16725 PMID: 39016108
- Yinhua Ni, .et al. , J Nutr Biochem, 2024, Mar:125:109569 PMID: 38185346
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Nahla E. El-Ashmawy, .et al. , Clin Phytosci, 2022, 8: 20
- Ming-Chun Hung, .et al. , Cell Biosci, 2022, 12: 122 PMID: 35918763
- Chien-Feng Li, .et al. , Cell Oncol (Dordr), 2021, Aug 2 PMID: 34339014
- Hiroharu Sakai, .et al. , Exp Ther Med, 2021, March 5 PMID: 33747195
- Cheng Zhou, .et al. , Cell Death Dis, 2021, Mar 3;12(3):231 PMID: 33658491
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- Lv H, .et al. , J Cell Physiol, 2018, Oct 26 PMID: 30362547
- Hui Liang, .et al. , Sci Rep, 2017, 7: 40361 PMID: 28098170
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CK2 inhibitor
CX-4945 is a potent and selective orally bioavailable small molecule inhibitor of CK2 that inhibits human umbilical vein endothelial cell migration, tube formation, and blocks CK2-dependent hypoxia-induced factor 1 alpha (HIF-1α) transcription in cancer cells.- Michael Ohene-Nyako, .et al. , ASN Neuro, 2023, Jan-Dec;15:17590914231158218 PMID: 36890725
- Wenjie Huang, .et al. , Am J Pathol, 2023, May;193(5):567-578 PMID: 37080661
- Xixi Zhao, .et al. , Cancer Res, 2022, Jun 6;82(11):2185-2195 PMID: 35385574
- Janeen H. Trembley, .et al. , Biomedicines, 2021, May; 9(5): 571 PMID: 34070147
- Tianzhi Huang, .et al. , Mol Cell, 2021, Mar 18;81(6):1276-1291 PMID: 33539787
- M Afzal, .et al. , Molecular and Cellular Biochemistry, 2020, 470, pages131-143
- Zaman MS, .et al. , Biometals, 2019, Oct 3 PMID: 31583500
- Fukumoto Y, .et al. , Biochem Biophys Res Commun, 2019, Sep 17;517(2):310-316 PMID: 31353086
- Fukumoto Y, .et al. , Biochem Biophys Res Commun, 2018, Oct 2;504(2):380-386 PMID: 29902452
- ST Ribeiro, .et al. , Leukemia, 2017, Jul; 31(7): 1603-1610 PMID: 27899804
- Valentina Gandin, .et al. , Nat Commun, 2016, 7: 11127 PMID: 27040916
- Ampofo E, .et al. , Eur Surg Res, 2016, 57(1-2):111-24 PMID: 27287005
- Emmanuel Ampofo, .et al. , Thromb Res., 2015, Nov;136(5):996-1006 PMID: 26381437
- Emmanuel Ampofo, .et al. , Biochim Biophys Acta., 2015, Oct;1852(10 Pt A):2123-36 PMID: 26189586
- A. Margarida Gomes, .et al. , Haematologica, 2014, 99(6): 1062-1068 PMID: 24561792
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CDK inhibitor
Kenpaullone is a potent inhibitor of CDK inhibitor (IC50 values are 0.4, 0.68, 7.5, 0.85 µM for CDK1/cyclinB, CDK2/cyclinA, CDK2/cyclinE and CDK5/p25 respectively). Also inhibits GSK-3β and LCK (IC50 values are 0.23 and 0.47 µM respectively) Displays reduced activity for other kinases (IC50 values are 15, 20, 20, 9 µM for c-src, casein kinase 2, ERK1 and ERK2 respectively). Also Generates iPSCs. Displays antiproliferative properties.
- Katelyn M Green, .et al. , J Biol Chem, 2019, jbc.RA119.009951
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Casein kinase inhibitor
Potent and selective casein kinase 1ε (CK1ε) and CK1δ inhibitor (IC50 values are 7.7 and 14 nM respectively) that displays > 30-fold selectivity over 42 other common kinases. Inhibits PER protein nuclear translocation (EC50 = 290 nM) causing phase shifts in circadian rhythms and attenuates methamphetamine-stimulated locomotion in vivo. -
Epidermal keratinocyte differentiation inducer
Casein Kinase II Inhibitor IV is a small-molecule inducer of epidermal keratinocyte differentiation. -
PKA, PKG, Casein Kinase I and II inhibitor
A-3 Hydrochloride is an inhibitor of PKA (cAMP-dependent protein kinase, Ki=4.3μM) and cGMP-dependent protein kinase, Ki=3.8μM, PKC (protein kinase C, Ki=47μM), casein kinase I and II, and MLCK (myosin light chain kinase) ( Ki=7.4μM). -
CK2 inhibitor
TTP 22 is a high affinity, casein kinase 2 (CK2) inhibitor (IC50= 0.1uM, Ki= 40nM). In addition, TTP 22 shows selectivity for CK2 over JNK3, ROCK1, and MET (inhibitory effects displayed at greater than 10 uM). TTP 22 is highly conserved serine/threonine protein kinase that is also involved in cell proliferation, cell differentiation and apoptosis. -
CK2 Inhibitor
TBB is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2)with IC50s of 0.9 and 1.6 uM for rat liver and human recombinant CK2 respectively).- Betsy T Kren, .et al. , Mol Med, 2024, Oct 11;30(1):175 PMID: 39394061
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CK2 inhibitor
CX-4945 sodium salt is a potent and selective ATP-competitive small molecule protein kinase CK2 inhibitor with a Ki and an IC50 of 0.38 and 1 nM for recombinant human CK2α, respectively. -
Casein kinase 1ε inhibitor
PF-4800567 is a potent and selective inhibitor of casein kinase 1ε (CK1ε), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). -
CK1δ/ε inhibitor
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. -
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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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. -
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. -
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. -
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. -
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. -
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. -
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.
