TGF-β/Smad

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  1. 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.
  2. 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.
  3. 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.
  4. PKC Activator

    1,2-Dimyristoyl-sn-glycerol is a saturated diacylglycerol that acts as a weak second messenger for the activation of Protein Kinase C (PKC). This compound is utilized in research applications to study PKC signaling pathways, which are crucial in various cellular processes including growth, differentiation, and apoptosis. As a PKC activator, it can help elucidate the role of PKC in different biological contexts and disease models.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. Anti-CD73/TGF-β Antibody

    Dalutrafusp alfa is a bifunctional antibody that targets CD73 and TGF-β, key components involved in the immunosuppressive pathway. This compound modulates immune responses by inhibiting adenosine production and blocking TGF-β signaling. It is primarily utilized in research focused on tumor immunology and the modulation of immune checkpoints. Its unique mechanism allows for exploration in various therapeutic applications, particularly in cancer treatment and autoimmune diseases.
  12. p32-kinase activator

    D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
  13. 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).
  14. 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.
  15. 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.
  16. 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.
  17. 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).

  18. BMP receptor inhibitor

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

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

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

    RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer.
  22. 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).
  23. PKCδ activator

    Roy-Bz is a selecive PKCδ activator. Roy-Bz potently inhibits the proliferation of colon cancer cells by inducing a PKCδ-dependent mitochondrial apoptotic pathway involving caspase-3 activation.
  24. 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).
  25. PKC inhibitor

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

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

    Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM.
  28. 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).
  29. 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).
  30. 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.
  31. 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.)
  32. PKC activator

    Prostratin is a protein kinase C activator found in the bark of the mamala tree of Samoa, Homalanthus nutans.
  33. ROCK Inhibitor

    HA-1077 inhibits vascular smooth muscle contraction by acting as an intracellular Ca2+ antagonist.
  34. 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.
  35. TGF-beta receptor inhibitor

    N/A
  36. BMP receptor inhibitor

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

    NH125 is a selective eEF-2 kinase inhibitor.
  38. 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.
  39. Valrubicin is a semisynthetic derivative of the antineoplastic anthracycline antibiotic doxorubicin.
  40. 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.
  41. 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).
  42. TGFβRI inhibitor

    BIBF0775 is an inhibitor of the transforming growth factor β receptor I (TGFβRI).
  43. protein kinase A activator

    8-Bromo-cAMP is a cell perbeable cyclic AMP (cAMP) analog and a PKA activator.
  44. ROCK inhibitor

    SAR407899 is a potent and selective Rho kinase inhibitor with promising antihypertensive activity.
  45. PKA inhibitor

    KT 5720 is prepared by a modificiation of K-252a (sc-200517), which is synthesized by the fungus Nocardiopsis sp.
  46. PKA-selective activator

    6-Bnz-cAMP is a PKA-selective activator. It regulates the PKA dependent signaling pathways.
  47. reversible PKA inhibitor

    Rp-cAMPS is a cell-permeable and reversible inhibitor of PKA (protein kinase A) (Ki = 11 uM). Rp-cAMPS is resistant to hydrolysis by phosphodiesterases and is noncompetitive with respect to ATP.
  48. PKG/PKA inhibitor

    cGMP Dependent Kinase Inhibitor Peptid is a specific cGKI (cyclic GMP-dependent protein kinase) inhibitor. Data indicates that it does not block cyclic GMP-dependent protein kinase phosphorylation of intact histones and has been used to study Plasmodium falciparum.
  49. TGF-β inhibitor

    (+)-ITD-1 is a resolved enantiomer of ITD-1 that possesses a greater than 2-fold increase in TGF-β inhibition (~400 nM) and 1.3-fold increase in cardiogenesis compared to the racemic ITD-1.
  50. ALK2 inhibitor

    LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM.

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