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TGF-β/Smad

Items 1-50 of 140

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  1. A10196
    Chelerythrine Chloride

    PKC inhibitor

    Chelerythrine affects translocation of PKC from cytosol to plasma membrane. Shown to prevent neurite growth. Induces apoptosis in a concentration- and schedule-dependent manner.

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  2. A10261
    Bryostatin 1

    PKC inhibitor

    Bryostatin 1 is a macrolactone isolated from the marine bryozoan, Bugula neritina, that modulates protein kinase C (PKC) activity. Bryostain 1 induces an initial rapid activation and autophosphorylation of PKC that results in the translocation of the PKC enzyme to the membrane.
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  3. A10286
    Daphnetin

    EGFR, PKA,PKC inhibitor

    Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent.
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  4. A10356
    LY317615 (Enzastaurin)

    PKCβ inhibitor

    LY317615 (Enzastaurin) is a potent and selective inhibitor of PKCβ with antiproliferative activity (IC50= ~6 nM).
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  5. A10381
    Fasudil HCl (HA-1077)

    ROCK inhibitor

    Fasudil HCl is a cyclic nucleotide-dependent protein kinase inhibitor and Rho-associated kinase inhibitor (IC50 = 10.7 μM).
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  6. A10441
    GSK429286A

    ROCK Inhibitor

    GSK429286A is a cell-permeable, selective small molecule inhibitor of Rho-associated, coiled-coil containing protein kinase (ROCK).
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  7. A10449
    Hesperetin

    PDE4 inhibitor

    Hesperetin, a selective phosphodiesterase (PDE)4 inhibitor, is present in the traditional Chinese medicine, ?€?Chen Pi.?€? Hesperetin is a citrus flavonoid that has been reported to lower plasma cholesterol. Hesperetin reduces the transcription of ACAT-2 mRNA in Hep-G2 cells and reduces ApoB protein synthesis in a dose-dependent manner. It also is a potential therapy for carcinoid cancer.
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  8. A10616
    Myricitrin (Myricitrine)

    Myricitrin is the 3-O-rhamnoside of myricetin. Myricitrin is used by several beetle species in their communication system.
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  9. A10766
    Quercetin (Sophoretin)

    MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
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  10. A10826
    SB 431542

    TGF-beta/Smad inhibitor

    SB 431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I ALK receptors ALK4, ALK5, and ALK7 .
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  11. A10827
    SB 525334

    ALK Inhibitor

    SB525334 is a selective inhibitor of transforming growth factor-β receptor I (ALK5, TGF-βRI) (IC50 = 14.3 nM). Inhibits TGF-β1-induced smad2/3 nuclear localization and TGF-βRI-induced mRNA expression in kidney cells
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  12. A10864
    Staurosporine

    PKC inhibitor

    Staurosporine is a natural product originally isolated in 1977 from the bacterium Streptomyces staurosporeus. The main biological activity of staurosporine is the inhibition of protein kinases through the prevention of ATP binding to the kinase. This is achieved through the stronger affinity of staurosporine to the ATP-binding site on the kinase.
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  13. A10899
    RKI-1313

    ROCK inhibitor

    RKI-1313 is a negative control for RKI-1447 which is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer.
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  14. A10928
    Thiazovivin

    ROCK inhibitor

    Thiazovivin is a selective inhibitor of Rho-associated kinase (ROCK).
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  15. A11001
    Y-27632 2HCl

    ROCK Inhibitor

    Y-27632 is a Rho-Associated Coil Kinase (ROCK) inhibitor that increases the cloning efficiency of human embryonic stem cells (hESCs).
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  16. A11017
    LY2157299

    TGF-βR Inhibitor

    LY2157299 is an orally active transforming growth factor beta receptor (TGF-βR) kinase inhibitor.
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  17. A11034
    A-674563

    Akt inhibitor

    A-674563 is a B/Akt inhibitor with an IC50 of 14 nM and also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively.
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  18. A11083
    GW788388

    TGF-beta/Smad inhibitor

    GW788388 is a potent, orally active and selective inhibitor of transforming growth factor beta receptor I (TGF-βR1) (activin receptor-like kinase 5, ALK5).
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  19. A11133
    LY2109761

    TβRI/II kinase inhibitor

    LY2109761, a novel transforming growth factor β receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis
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  20. A11157
    SB-505124

    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).
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  21. A11205
    LDN193189

    ALK inhibitor

    LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.
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  22. A11478
    LDN193189 HCl

    LDN193189 HCl is the hydrochloride salt of LDN193189. LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.
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  23. A11554
    Sotrastaurin (AEB071)

    PKC inhibitor

    Sotrastaurin is a protein kinase C inhibitor for the prevention of transplant rejection and treatment of psoriasis.
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  24. A11610
    Y-33075

    ROCK inhibitor

    Y-33075 is ROCK (Rho-associated coiled coil-forming protein kinase) inhibitor.
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  25. A11611
    Y-33075 dihydrochloride

    ROCK inhibitor

    Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM.
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  26. A11762
    RepSox (SJN 2511)

    ALK5 inhibitor

    RepSox (SJN 2511) is a selective inhibitor of the TGF-β type I receptor ALK5 (IC50 values are 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding respectively).
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  27. A11935
    H 89 2HCl

    PKA inhibitor

    H 89 dihydrochloride is a cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase.
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  28. A12014
    Verbascoside

    PKC inhibitor

    Verbascoside is isolated from Lantana camara, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 μM, and has antitumor, anti-inflammatory and antineuropathic pain activity.
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  29. A12304
    D-erythro-Sphingosine

    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.
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  30. A12348
    GSK 269962

    ROCK inhibitor

    GSK 269962 is a potent Rho kinase (ROCK) inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively).
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  31. A12358
    A 83-01

    TGF-β/ALK5 inhibitor

    A83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor ALK7
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  32. A12399
    Ruboxistaurin (LY333531)

    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).
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  33. A12419
    Go 6976

    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.
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  34. A12464
    AT13148

    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.
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  35. A12650
    PKC 412 (Midostaurin)

    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.
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  36. A12674
    SR 3677 dihydrochloride

    ROCK inhibitor

    SR 3677 dihydrochloride is a potent and selective Rho-kinase inhibitor (IC50 values are 3 and 56 nM for ROCK-II and ROCK-I respectively).
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  37. A12820
    DMH-1

    ALK2 inhibitor

    DMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM).
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  38. A12821
    LDN-212854

    BMP receptor inhibitor

    LDN-212854 is an ALK2-Biased BMP Type I Receptor Kinase Inhibitor.
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  39. A12829
    Delcasertib

    δ-protein kinase C (δPKC) inhibitor

    Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor.
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  40. A12924
    ITD-1

    TGF-β inhibitor

    ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells.
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  41. A12926
    Kartogenin

    Smad inhibitor

    Kartogenin potently induces differentiation of human mesenchymal stem cells into chondrocytes
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  42. A12963
    Ingenol Mebutate (PEP005)

    Ingenol mebutate is a substance found in the sap of the plant Euphorbia peplus and an inducer of cell death.
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  43. A13043
    (-)-Indolactam V

    PKC activator

    (-)-Indolactam V is a protein kinase C activator, which strongly directs human ES cell-derived definitive endoderm into pancreatic endoderm.
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  44. A13067
    RKI-1447

    ROCK1/ROCK2 inhibitor

    RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer.
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  45. A13094
    alpha-Amyloid Precursor Protein Modulator

    alpha-Amyloid Precursor Protein Modulator is a cell-permeable benzolactam derived PKC activator (Ki = 11.9 nM for PKCα) that efficiently enhances non-amyloidogenic α-processing of amyloid precursor protein (APP) even at 100 nM in human fibroblas.
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  46. A13197
    GF 109203X

    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).
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  47. A13348
    Roy-Bz

    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.
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  48. A13446
    LY364947

    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).
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  49. A13514
    Ro 31-8220 mesylate

    PKC inhibitor

    Ro 31-8220 mesylate is a PKC-inhibitor, which inhibits stimulated fluid pinocytosis of human PMNs induced by the PKC-activators phorbol myristate acetate (PMA, IC50 = 1.35 x 10(-6) M) or diacylglycerols (OAG, diC8) by 95%.
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  50. A13584
    A-3 Hydrochloride

    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).
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