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Catalog No.
Product Name
Application
Product Information
Citations
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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
- Daniel Limonta, .et al. , J Infect Dis, 2019, 2019 PMID: 30799482
- 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. -
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. -
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. -
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). -
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. -
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 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. -
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. -
Selective p38α Inhibitor
AMG-548 dihydrochloride is a selective p38α inhibitor with a Ki of 0.5 nM, exhibiting moderate selectivity towards p38β (Ki = 36 nM) and over 1000-fold selectivity against p38γ and p38δ isoforms. This compound demonstrates potent inhibition of TNFα production in whole blood stimulated by LPS, with an IC50 of 3 nM. Additionally, AMG-548 dihydrochloride inhibits Wnt signaling by directly targeting Casein kinase 1 isoforms δ and ε, making it valuable for research in inflammation and signaling pathways. -
CK2 Inhibitor
(E/Z)-GO289 is a potent and selective inhibitor of casein kinase 2 (CK2) with an IC50 of 7 nM. This compound significantly extends the circadian period and demonstrates cell type-dependent inhibition of cancer cell growth, which correlates with cellular clock function. (E/Z)-GO289 is valuable for research into circadian biology and cancer therapeutics. -
CK1 Inhibitor
CKI-7 free base is a selective casein kinase 1 (CK1) inhibitor that operates through an ATP-competitive mechanism, exhibiting an IC50 of 6 μM and a Ki of 8.5 μM. In addition to its primary action on CK1, CKI-7 also inhibits Cdc7 kinase, SGK, ribosomal S6 kinase-1 (S6K1), and mitogen- and stress-activated protein kinase-1 (MSK1). This compound demonstrates minimal activity against casein kinase II and other protein kinases, making it a valuable tool for research applications focused on cell cycle regulation and signal transduction pathways. -
CSNK1α Inhibitor
BAY-204 is a selective inhibitor of casein kinase 1 alpha (CSNK1α), functioning through ATP-competitive mechanisms with an IC50 of 2 nM at 10 μM ATP and 12 nM at 1 mM ATP. This compound is primarily utilized in research focused on acute myeloid leukemia (AML), providing valuable insights into the role of CSNK1α in cancer biology and potential therapeutic interventions. -
CSNK1A1/CSNK1D Inhibitor
BAY-888 is a selective inhibitor of casein kinase 1α (CK1α/CSNK1A1) that acts through ATP-competitive mechanisms, exhibiting an IC50 of 4 nM at 10 μM ATP and 63 nM at 1 mM ATP. This compound disrupts the negative regulatory effects of CK1α on p53 and other associated signaling pathways, thereby inducing apoptosis and inhibiting tumor cell proliferation. BAY-888 has demonstrated efficacy against various cancers, including acute myeloid leukemia (AML), and is utilized in research focused on the development of anticancer therapeutics for p53 wild-type tumors and exploring mechanisms in CK1α-related signaling pathways. -
CK1 Inhibitor
CK1-IN-2 is a selective inhibitor of casein kinase 1 (CK1) with demonstrated IC50 values of 123 nM for CK1α, 19.8 nM for CK1δ, 26.8 nM for CK1ε, and 74.3 nM for p38α. This compound exhibits significant inhibition of CK1 activity, making it a valuable tool for dissecting CK1-mediated signaling pathways. CK1-IN-2 is useful in oncology and neurobiology research, particularly in studies exploring cell proliferation, apoptosis, and circadian rhythm regulation. -
CK2 Inhibitor
CK2 Inhibitor 2 targets Casein Kinase 2 (CK2) and acts as a potent, selective inhibitor with an IC50 of 0.66 nM. This compound demonstrates a high degree of selectivity for CK2, exhibiting an IC50 of 32.69 nM against Clk2. CK2 Inhibitor 2 has been shown to exert significant antiproliferative and antitumor effects, making it a valuable tool for research related to cancer biology and signal transduction. -
Casein Kinase Inhibitor
TBCA is a selective inhibitor of casein kinase II (CK2), exhibiting an IC50 of 110 nM and a Ki value of 77 nM. This compound demonstrates a significant preference for CK2 over CK1, DYRK1A, and a diverse panel of 27 other kinases. TBCA is valuable for research applications focused on studying the role of CK2 in cellular signaling and disease mechanisms. -
Casein Kinase Inhibitor
PI-828 is a dual inhibitor of phosphoinositide 3-kinase (PI3K) and casein kinase 2 (CK2), exhibiting IC50 values of 173 nM for p110α, 149 nM for CK2, and 1127 nM for CK2α2 in lipid kinase assays. This compound demonstrates significant biological activity by modulating key signaling pathways involved in cell growth and survival. PI-828 is utilized in research applications focused on cancer biology, providing insights into tumorigenesis and potential therapeutic interventions targeting these kinases. -
CSNK2A Inhibitor
CSNK2A-IN-1 is a selective inhibitor of Casein Kinase 2 Alpha (CSNK2A), a crucial regulator in various cellular processes. This compound exhibits antiviral activity and demonstrates improved selectivity compared to other kinases, such as PIM3. CSNK2A-IN-1 is relevant for research applications involving studies of viral pathogenesis and kinase signaling pathways. -
CK2α Inhibitor
CK2α-IN-1 is a selective inhibitor of casein kinase 2 alpha (CK2α) with an IC50 value of 7.0 µM and a Ki of 1.6 µM. This compound operates through a non-ATP-competitive mechanism, making it a valuable tool for investigating CK2α's role in cellular regulation. CK2α-IN-1 shows promising potential for anticancer research applications, providing insights into cancer cell proliferation and survival pathways.
