Casein Kinase

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  1. TBB

    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).
  2. PI3K Inhibitor

    LY294002 is a PI3k inhibitor (cell IC50 about 10 μM) and a casein kinase II inhibitor.
  3. 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.

  4. 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.
  5. 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

  6. 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.
  7. Epidermal keratinocyte differentiation inducer

    Casein Kinase II Inhibitor IV is a small-molecule inducer of epidermal keratinocyte differentiation.
  8. CK1 inhibitor

    LH 846 is a selective inhibitor of casein kinase (CK) 1δ (IC50 values are 290 nM, 1.3 μM and 2.5 μM for CK1δ, ε and α)
  9. 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).
  10. CK1 Inhibitor

    D4476 is a cell-permeant inhibitor of casein kinase 1.
  11. CK2/ERK8 inhibitor

    MCB has been shown to inhibit both casein kinase 2 (CK2) and extracellular-signal-regulated kinase 8 (ERK8/MAPK15) (IC50 = 0.50 uM for both CK2 and ERK8).
  12. 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.
  13. CK1δ and CK1ε inhibitor

    IC 261 is CK1δ and CK1ε inhibitor.
  14. 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.
  15. CK1δ/CK1ε inhibitor

    SR-3029 is a potent and highly specific CK1δ/CK1ε inhibitor with the IC50 of 97 nM.
  16. CK inhibitor

    TA-01 potently inhibits CK1ε, CK1δ,and p38α (IC50values are 6.4, 6.8, and 6.7 nM respectively).
  17. 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).
  18. 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.
  19. CK1 inhibitor

    CK1-IN-1 is a casein kinase 1 (CK1) inhibitor extracted from patent WO2015119579A1, compound 1c, has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38?? MAPK, respectively.
  20. CK2 inhibitor

    DMAT is a potent and specific CK2 inhibitor with an IC50 of 0.13 uM.
  21. CK2 Peptide Substrate

    CK2 Substrate Peptide (RRRADDSDDDDD) serves as a specific substrate for Casein Kinase 2 (CK2), exhibiting a Km of 13 μM. This peptide is crucial for studying CK2's role in various biological processes and provides valuable insights into the mechanisms underlying neurological diseases, including Alzheimer's Disease. Research applications include elucidating CK2-mediated phosphorylation events and investigating potential therapeutic targets.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. PDE6D/CK1α Degrader

    TMX-4113 is a degrader targeting phosphodiesterase 6D (PDE6D) and casein kinase 1α (CK1α). This compound exhibits significant biological activity in the degradation of these proteins, making it a valuable tool for investigating their roles in cancer research. TMX-4113 can facilitate studies aimed at elucidating the molecular mechanisms underlying tumor progression and treatment responses.
  32. 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.
  33. 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.
  34. CSNK1D/CSNK1E Inhibitor

    JNJ-6204 is a potent dual inhibitor of Casein Kinase 1 Delta (CSNK1D) and Casein Kinase 1 Epsilon (CSNK1E), with IC50 values of 2.3 nM and 137 nM, respectively. This compound exhibits significant brain penetration, making it a valuable tool for investigating the roles of CSNK1D and CSNK1E in cellular signaling and neurobiology. JNJ-6204 is particularly useful in the study of diseases associated with dysregulated Wnt signaling and circadian rhythm disturbances.
  35. CK-1δ Inhibitor

    Casein kinase 1δ-IN-6 is a selective inhibitor of protein kinase CK-1δ, demonstrated by an IC50 of 23 nM. This compound exhibits neuroprotective and anti-inflammatory effects, both in vitro and in vivo, making it a valuable tool for studying neurodegenerative diseases. Its specific mechanism of action and ability to modulate CK-1δ activity position it as a promising candidate for therapeutic research.
  36. CK2/SRPK1 Dual Inhibitor

    SRPIN803 is a dual inhibitor of casein kinase 2 (CK2) and serine/arginine-rich protein-specific kinase 1 (SRPK1), with IC50 values of 203 nM and 2.4 μM, respectively. This compound demonstrates antiangiogenic properties, making it a valuable tool for studies related to angiogenesis. SRPIN803 is particularly relevant for researching therapeutic strategies in age-related macular degeneration and other conditions influenced by vascular growth.
  37. CK1/CDK1/CDK5 Inhibitor

    (R)-DRF053 dihydrochloride is a selective inhibitor of casein kinases 1 (CK1), CDK1/cyclin B, and CDK5/p25, exhibiting IC50 values of 14 nM, 220 nM, and 80 nM, respectively. This compound effectively inhibits the CK1-mediated generation of amyloid-beta in cellular models, making it valuable for research into neurodegenerative diseases and cellular signaling pathways. Its specificity and potency position it as a suitable reagent for investigating the roles of these kinases in various biological processes.
  38. CK2 Inhibitor

    CK2-IN-10 is an allosteric inhibitor of casein kinase 2 (CK2), known for its role in cellular signaling and proliferation. This compound demonstrates significant potential in cancer research by inhibiting CK2 activity, which is often dysregulated in various malignancies. CK2-IN-10 can be utilized in studies focusing on cancer cell growth, survival mechanisms, and therapeutic resistance, making it a valuable tool for advancing cancer biology research.
  39. CK1d Inhibitor

    Casein kinase 1δ-IN-3 is a selective inhibitor of casein kinase 1 delta (CK1d) with a pIC50 of 6.5376 M. This compound is instrumental in studying CK1d's role in various biological processes, including circadian rhythm regulation and signaling pathways. Its inhibitory activity makes it a valuable tool for investigating CK1d-related functions in cellular and molecular research.
  40. CK1/CHK1 Inhibitor

    MRT00033659 is a selective inhibitor targeting casein kinase 1 (CK1) and checkpoint kinase 1 (CHK1), with IC50 values of 0.9 μM and 0.23 μM, respectively. As a pyrazolo-pyridine analogue, MRT00033659 activates the p53 signaling pathway and causes destabilization of E2F-1. This compound is valuable for research investigating cell cycle regulation, DNA damage response, and therapeutic strategies in cancer biology.
  41. CK1α Degrader

    CK1α degrader-1 is a selective degrader of casein kinase 1 alpha (CK1α) that exhibits a DC50 of 0.105 μM. This compound effectively promotes the degradation of CK1α, thereby influencing cellular signaling pathways related to cancer progression. It serves as a valuable tool for investigating the role of CK1α in cancer biology and therapeutic interventions.
  42. Casein kinase 1δ Inhibitor

    Casein kinase 1δ-IN-8 is an inhibitor of Casein kinase 1δ, a serine/threonine kinase implicated in various cellular processes. This compound is valuable for research into neurodegenerative disorders, including Alzheimer's disease, by elucidating the role of Casein kinase 1δ in disease pathology and potential therapeutic interventions. Its selective inhibition allows for targeted studies of kinase activity and its downstream effects in relevant biological systems.
  43. CK1δ Inhibitor

    Casein kinase 1δ-IN-1 is a selective inhibitor of casein kinase 1δ (CK1δ), which plays a crucial role in various cellular processes. This compound exhibits significant biological activity in modulating CK1δ signaling pathways, making it a valuable tool for investigating the mechanisms underlying neurodegenerative diseases, particularly tauopathies. Researchers can utilize Casein kinase 1δ-IN-1 to explore its effects on tau phosphorylation and the potential therapeutic implications for related disorders.
  44. CK2 Inhibitor

    CK2-IN-4 is a selective inhibitor of casein kinase 2 (CK2), with an IC50 of 8.6 µM. This compound exhibits significant potential for investigating its role in cancer progression, viral pathogenesis, and glomerulonephritis. Researchers can utilize CK2-IN-4 to study the mechanisms underlying CK2-related signaling pathways and to explore therapeutic avenues in related diseases.
  45. CKIα/δ Inhibitor

    NCC007 is a dual inhibitor of casein kinases Iα (CKIα) and δ (CKIδ), demonstrating IC50 values of 1.8 μM and 3.6 μM, respectively. This compound is effective in modulating mammalian circadian rhythms, making it a valuable tool in chronobiology research. Its use can facilitate studies aimed at understanding the molecular mechanisms underlying circadian regulation and potential therapeutic interventions for circadian-related disorders.
  46. CK1δ/ε Inhibitor

    SR-1277 is a potent and selective inhibitor of casein kinase 1 delta (CK1δ) and epsilon (CK1ε), demonstrating ATP-competitive inhibition with IC50 values of 49 nM and 260 nM, respectively. Additionally, it exhibits inhibitory effects on FLT3, CDK4/cyclin D1, CDK6/cyclin D3, and CDK9/cyclin K, with IC50 values of 305 nM, 1340 nM, 311 nM, and 109 nM, respectively. SR-1277 is primarily employed in cancer research, contributing to studies investigating CK1-mediated signaling pathways and therapeutic potential.
  47. Casein Kinase Inhibitor

    Casein Kinase II Inhibitor IV hydrochloride is a selective inhibitor of Casein Kinase II (CK2), a serine/threonine kinase involved in various cellular processes. This compound promotes differentiation in epidermal keratinocytes, making it valuable for research on skin biology and related disorders. Additionally, it can be used to explore the roles of CK2 in cell proliferation, apoptosis, and signaling pathways.
  48. PI3Kδ/CK1ε Inhibitor

    Umbralisib tosylate is a potent and selective dual inhibitor of PI3Kδ and casein kinase-1-ε (CK1ε), exhibiting an EC50 of 22.2 nM and 6.0 μM, respectively. This compound demonstrates significant immunomodulatory effects on T cells from chronic lymphocytic leukemia (CLL) patients. Umbralisib tosylate is primarily utilized in research focused on hematological malignancies to elucidate its therapeutic potential and mechanisms of action.
  49. PI3Kδ/CK1ε Inhibitor

    Umbralisib sulfate is a potent and selective dual inhibitor of PI3Kδ and casein kinase-1-ε (CK1ε), with EC50 values of 22.2 nM and 6.0 μM, respectively. This compound demonstrates notable immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL). Umbralisib sulfate is a valuable tool for research into hematological malignancies, facilitating studies on cell signaling pathways and potential therapeutic strategies.
  50. CK1 Inhibitor

    PF-4800567 hydrochloride is a potent and selective inhibitor of casein kinase 1 (CK1), exhibiting an IC50 of 32 nM. It demonstrates over 20-fold selectivity for CK1α when compared to CK1δ, with an IC50 value of 711 nM. This compound is valuable for investigating the distinct roles of these kinases in various signaling pathways, making it an essential tool for research in cellular signaling and kinase-related studies.

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