TGF-β/Smad

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  1. PKC Inhibitor

    N-Myristoyl-Lys-Arg-Thr-Leu-Arg is a selective inhibitor of protein kinase C (PKC), exhibiting an IC50 of 75 μM. This compound effectively inhibits the induction of the IL-2 receptor and production of IL-2 in the Jurkat human leukemic cell line. It can be utilized in research focused on understanding PKC-related signaling pathways and their role in immune responses.
  2. PKC-θ Inhibitor

    PKC-theta inhibitor 2 hydrochloride is a highly selective inhibitor of protein kinase C theta (PKC-θ), exhibiting an IC50 of 18 nM. This compound modulates key signaling pathways associated with T cell activation and proliferation. It serves as a valuable tool in research investigating autoimmune diseases, cancer therapeutics, and immune response modulation.
  3. PKC Inhibitor

    Safingol is a lyso-sphingolipid that acts as a selective protein kinase C (PKC) inhibitor. It has demonstrated potential in modulating various cellular signaling pathways, making it an important tool in cancer research and studies of cell survival and apoptosis. Safingol is valuable for investigating the role of PKC in diseases and may aid in the development of therapeutic strategies targeting this kinase.
  4. OPN4 Inhibitor

    AE 51310 is an inhibitor of the OPN4 receptor, effectively disrupting the activation of protein kinase C (PKC) and the downstream BRAF/MEK/ERK signaling cascade. This compound is valuable for cancer research, particularly in the study of non-small cell lung cancer (NSCLC). Its ability to modulate critical signaling pathways makes AE 51310 a useful tool in investigating tumor biology and potential therapeutic targets.
  5. PKC-ι Inhibitor

    PKCiota-IN-1 is a potent inhibitor of protein kinase C iota (PKC-ι) with an IC50 of 2.7 nM. This compound also exhibits inhibitory activity against PKC-α and PKC-ε, with IC50 values of 45 nM and 450 nM, respectively. PKCiota-IN-1 is valuable for studying the role of PKC-ι in various biological processes and has potential applications in cancer research and therapeutic strategies targeting PKC pathways.
  6. PKC Inhibitor

    CIDD-0072424 is a selective inhibitor of Protein Kinase C-epsilon (PKCε), exhibiting an inhibitory constant (Ki) of 54 nM. This compound has been shown to reduce ethanol consumption and preference in a dose-dependent manner, making it a valuable tool for studying alcohol-related behaviors and signaling pathways. It is applicable in research investigating the role of PKCε in addiction and other neurobiological processes.
  7. PKC Inhibitor

    MT477 is a potent protein kinase C (PKC) inhibitor that induces both apoptosis and necrosis in target cells. This compound effectively reduces the protein expression levels of Ras-GTP, p-Erk1/2, and p-Elk1. Due to its mechanism of action, MT477 demonstrates significant antitumor activity, making it a valuable tool for cancer research and therapeutic investigations.
  8. PKC Inhibitor

    PKC-IN-5, a protein kinase C (PKC) inhibitor, disrupts the interaction between PKC epsilon (PKCe) and its adaptor protein RACK2. This inhibition can modulate PKC-mediated signaling pathways, making PKC-IN-5 a valuable tool for studying PKC-related cellular processes. Its application extends to research in cancer biology and neurodegenerative diseases, where PKC signaling plays a critical role.
  9. Protein Kinase C Inhibitor

    Ro 31-8830 is a potent and selective inhibitor of protein kinase C, which plays a crucial role in various cell signaling pathways. This compound demonstrates anti-inflammatory activity and is valuable for research focused on inflammatory disorders. Its capabilities make Ro 31-8830 a significant tool for investigating the mechanisms underlying inflammation and evaluating potential therapeutic strategies.
  10. PKC Inhibitor

    R8605 is a protein kinase C (PKC) inhibitor with a reported IC50 of 65 μM in the rat brain. This compound also inhibits calcium/phospholipid-independent phosphorylation of protamine, with IC50 values of 70 μM and 100 μM, respectively. R8605 is applicable in cancer research, facilitating studies on PKC-mediated signaling pathways and their implications in tumorigenesis.
  11. PKC Inhibitor

    Safingol hydrochloride is a lyso-sphingolipid that functions as a potent inhibitor of protein kinase C (PKC). This compound exhibits significant biological activity in modulating cellular signaling pathways associated with cancer progression and apoptosis. Safingol hydrochloride is primarily utilized in research focused on cancer biology, cardiovascular disease, and neuroprotection, providing valuable insights into PKC-related mechanisms.
  12. PKCβII Inhibitor

    PKCβII Peptide Inhibitor I is a selective inhibitor of Protein Kinase C beta II (PKCβII). This peptide demonstrates significant cardioprotective effects in rat models of ischemia/reperfusion injury, making it a valuable tool in cardiovascular research. Additionally, it has been shown to prevent vascular endothelial dysfunction, highlighting its potential applications in studying vascular health and related pathologies.
  13. Protein Kinase C Inhibitor/LTD4 Antagonist

    LY 170198 is a potent protein kinase C inhibitor and LTD4 antagonist. This compound exhibits significant biological activity relevant to studies on tumor promotion, oncogene activation, and protein phosphorylation. Additionally, it is valuable for investigating feedback mechanisms in signal transduction pathways and cellular responses to growth factors, making it a useful tool for cancer research and related fields.
  14. PKC Inhibitor

    Go 7874 is a protein kinase C (PKC) inhibitor that exhibits neuroprotective effects in models of immune-mediated neurotoxicity. This compound mitigates LPS/IFNg-induced neuronal cell death not through conventional PKC inhibition, but by suppressing the expression of inducible nitric oxide synthase (iNOS), leading to decreased nitric oxide (NO) production. Its unique mechanism makes Go 7874 a valuable tool for studying neuroprotective strategies in inflammatory conditions.
  15. Akt/ROCK Inhibitor

    Akt/ROCK-IN-1 is a potent dual inhibitor targeting Akt and ROCK, exhibiting IC50 values of 0.023 nM and 1.47 nM, respectively. This compound demonstrates significant antitumor activity, particularly in neuroblastoma models. It serves as a valuable tool for research into cancer biology and therapeutic development.
  16. PKCα Inhibitor

    Desmethylglycitein (4',6,7-Trihydroxyisoflavone) is an inhibitor of protein kinase C (PKC)α, demonstrating significant anti-cancer and antioxidant activities. It directly binds to CDK1 and CDK2, leading to the suppression of their activity. Additionally, Desmethylglycitein inhibits PI3K in an ATP-competitive manner, affecting downstream signaling pathways and reducing adipogenesis in 3T3-L1 preadipocytes. Its mechanisms make it a valuable tool for research in cancer biology and metabolic disorders.
  17. PKC Inhibitor

    Bisindolylmaleimide X is a potent protein kinase C (PKC) inhibitor that exhibits cell-penetrating properties. It effectively inhibits the proliferation of CD4 T cells in vitro and shows antagonistic activity against cyclin-dependent kinase 2 (CDK2) with an IC50 of 200 nM. Additionally, Bisindolylmaleimide X suppresses eNOS-Ser1177 phosphorylation in human embryonic vein endothelial cells. This compound is valuable for studying mechanisms in the immune system and cardiovascular diseases.
  18. PKA Anchoring Inhibitor

    st-Ht31 is a membrane-permeable peptide that inhibits protein kinase A (PKA) anchoring. It effectively induces cholesterol and phospholipid efflux and has been shown to completely reverse foam cell formation in macrophages. This compound offers valuable insights into PKA-related signaling pathways and metabolic health research.
  19. Myo1s/TGF-β Inhibitor

    Pentachloropseudilin is a potent reversible allosteric inhibitor targeting Myo1s (class 1 myosins), exhibiting IC50 values ranging from 1 to 5 μM for mammalian class-1 myosins, while displaying greater than 90 μM for class-2 and class-5 myosins. Additionally, it effectively inhibits transforming growth factor-β (TGF-β) signaling, with an IC50 of 0.1 to 0.2 μM. This compound is valuable for research in cellular signaling pathways and myosin function, contributing to studies in cell motility and tissue remodeling.
  20. PKC Inhibitor

    PKC-iota inhibitor 1 is an inhibitor of protein kinase C-iota (PKC-ι) with an IC50 value of 0.34 μM. This compound demonstrates significant biological activity relevant to cancer research, making it a valuable tool for investigating the role of PKC-ι in tumorigenesis and signal transduction pathways. It is suitable for studies focused on cancer biology and therapeutic interventions targeting PKC-ι.
  21. PKC Inhibitor

    DL-erythro-Dihydrosphingosine is a sphingosine-derived protein kinase C (PKC) inhibitor that functions by directly inhibiting phospholipase A2 (PLA2) activity. This compound also attenuates the function of Bcl-2, a protein that plays a crucial role in regulating apoptosis. Additionally, DL-erythro-Dihydrosphingosine inhibits matrix metalloproteinases (MMPs), which are involved in various cellular processes. Its unique biological activity makes it valuable for research in cancer and inflammatory disease models.
  22. PKC/HCMV Inhibitor

    Bisindolylmaleimide IV is a selective inhibitor of protein kinase C (PKC), exhibiting IC50 values between 0.1 and 0.55 μM. It also demonstrates inhibition of protein kinase A (PKA) with IC50 ranging from 3.1 to 11.8 μM. In addition to its kinase inhibitory properties, Bisindolylmaleimide IV effectively inhibits human cytomegalovirus (HCMV) replication in cell culture, displaying an IC50 of 0.2 μM. This reagent is valuable for research applications focused on signal transduction and viral pathogenesis.
  23. PKC Inhibitor

    Sangivamycin is a nucleoside analog that serves as a potent inhibitor of protein kinase C (PKC) with a Ki value of 10 μM. This compound exhibits significant antiproliferative activity against a diverse range of human cancers, making it a valuable tool for cancer research and therapeutic studies focused on PKC modulation. Its targeted mechanism of action positions Sangivamycin as a promising candidate for further exploration in cancer treatment.
  24. PKC inhibitor

    Ruboxistaurin (LY333531) is a potent, selective inhibitor of Protein Kinase C isozymes, PKC β I(IC50=4.7 nM) and PKC β II (IC50=5.9 nM).
  25. PKC inhibitor

    Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
  26. multi-AGC kinase inhibitor

    AT13148 is a novel oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity, which shows a distinct mechanism of action from other AKT inhibitors.
  27. PKC inhibitor

    PKC 412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms α/β/γ, PDFRβ, VEGFR2, Syk, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity.
  28. ROCK inhibitor

    SR 3677  is a potent and selective Rho-kinase inhibitor (IC50 values are 3 and 56 nM for ROCK-II and ROCK-I respectively).

  29. BMP receptor inhibitor

    LDN-212854 is an ALK2-Biased BMP Type I Receptor Kinase Inhibitor.
  30. δ-protein kinase C (δPKC) inhibitor

    Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor.
  31. Smad inhibitor

    Kartogenin potently induces differentiation of human mesenchymal stem cells into chondrocytes
  32. ROCK1/ROCK2 inhibitor

    RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer.
  33. PKC inhibitor

    GF 109203X is a potent and selective inhibitor of protein kinase C, selective for the α and β1 isoforms (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Selective over MLCK, PKG and PKA (IC50 values are 0.6, 4.6, and 33 μM respectively). Potent antagonist at the 5-HT3 receptor (Ki = 29.5 nM).
  34. ALK5 inhibitor

    SB-505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5), ALK4 and ALK7 (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively).
  35. PKC inhibitor

    Sotrastaurin is a protein kinase C inhibitor for the prevention of transplant rejection and treatment of psoriasis.
  36. ROCK inhibitor

    Y-33075 is ROCK (Rho-associated coiled coil-forming protein kinase) inhibitor.
  37. ROCK inhibitor

    Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM.
  38. TGFβR-I Inhibitor

    LY364947 is a diheteroaryl-substituted pyrazole compound used as a selective, ATP-competitive inhibitor of TGF-βRI (TGF-β Receptor I kinase).
  39. 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).
  40. MAPKAP-K2 (MK-2) inhibitor

    MK-2 Inhibitor III (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM.
  41. ROCK inhibitor

    Glycyl-H 1152 2HCl is a selective and potent ROCK inhibitor (IC50 values are 0.0118, 2.35, 2.57, 3.26, > 10 and >10 uM for ROCKII, Aurora A, CAMKII, PKG, PKA and PKC respectively.)
  42. ROCK Inhibitor

    HA-1077 inhibits vascular smooth muscle contraction by acting as an intracellular Ca2+ antagonist.
  43. TGF-βR Inhibitor

    SD-208 is a potent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50= 49 nM); displays > 100-fold and > 17-fold selectivity over TGF-βRII and other common kinases respectively.
  44. TGF-beta receptor inhibitor

    N/A
  45. BMP receptor inhibitor

    ML347 is a selective BMP receptor inhibitor .
  46. eEF-2 inhibitor

    NH125 is a selective eEF-2 kinase inhibitor.
  47. BMP inhibitor

    K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6.
  48. ALK5 inhibitor

    A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.
  49. PKs inhibitor

    HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50 = 8, 12, and 4 μM, respectively).
  50. TGFβRI inhibitor

    BIBF0775 is an inhibitor of the transforming growth factor β receptor I (TGFβRI).

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