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TGF-β/Smad

Items 1-50 of 510

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  1. 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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  2. 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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  3. A15914
    Dibutyryl-cAMP

    PKA activator

    Dibutyryl-cAMP is a cell-permeable PKA activator by mimicing the action of endogenous cAMP.
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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. 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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  6. 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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  7. A14213
    EW-7197 (Vactosertib)

    ALK4/ALK5 inhibitor

    EW-7197 is a highly potent, selective, and orally bioavailable TGF-β I receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively
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  8. 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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  9. A16031
    PKI 14-22 amide, myristoylated

    PKA inhibitor

    PKI 14-22 amide, myristoylated is a useful heat stable cAMP-dependent protein kinase inhibitor. This is often used to study PKA in cellular systems in-vitro.
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  10. A15225
    Azaindole 1 (BAY-549)

    ROCK inhibitor

    Azaindole 1 (BAY-549) is a highly potent inhibitor of human ROCK-1 and ROCK-2 isoenzymes with IC50 values of 0.6 and 1.1 nM, respectively.

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  11. 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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  12. 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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  13. A13790
    GO6983

    PKC inhibitor

    GO6983 is a potent protein kinase C (PKC) inhibitor. It reduces polymorphonuclear leukocyte adherence and infiltration following myocardial ischemia/reperfusion injury.
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  14. 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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  15. 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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  16. 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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  17. 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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  18. 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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  19. 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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  20. A16065
    SIS3

    Smad3 inhibitor

    SIS3 is a novel specific inhibitor of Smad3. It has effect on transforming growth factor-beta1-induced extracellular matrix expression.
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  21. A16209
    Pirfenidone
    Pirfenidone is an anti-fibrotic drug for the treatment of idiopathic pulmonary fibrosis (IPF). It works by reducing lung fibrosis through downregulation of the production of growth factors and procollagens I and II.
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  22. A14616
    12-O-tetradecanoyl phorbol-13-acetate

    PKC activator

    12-O-tetradecanoyl phorbol-13-acetate is a diester of phorbol and is a tumor promoting compound extracted from croton oil. It is a reversible, highly potent protein kinase C (PKC) activator in vitro and in vivo at nM concentrations.
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  23. 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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  24. A21448
    Y-27632

    ROCK-I/ROCK-II inhibitor

    Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, respectively.
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  25. 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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  26. 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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  27. 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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  28. A12820
    DMH-1

    BMP inhibitor

    DMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM).
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  29. A15888
    Ripasudil

    ROCK inhibitor

    Ripasudil (K-115) is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.
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  30. 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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  31. 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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  32. 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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  33. 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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  34. 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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  35. A11017
    Galunisertib (LY2157299)

    TGF-βR Inhibitor

    LY2157299 is an orally active transforming growth factor beta receptor (TGF-βR) kinase inhibitor.
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  36. 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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  37. 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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  38. 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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  39. 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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  40. 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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  41. 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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  42. A10928
    Thiazovivin

    ROCK inhibitor

    Thiazovivin is a selective inhibitor of Rho-associated kinase (ROCK).
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  43. A23132
    Malantide
    Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.
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  44. A23135
    Protein Kinase C (19-31)
    Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
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  45. A24705
    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine

    Smad3/HIF-α Dual Target PROTAC

    (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine functions as a dual-target PROTAC, effectively inducing ubiquitination and degradation of Smad3 while simultaneously enhancing HIF-α protein levels. This compound exhibits multi-pathway anti-fibrotic activity and renal protective properties, making it valuable for research on renal anemia. Additionally, it has potential applications in studying prostate cancer and other malignancies, contributing to a deeper understanding of cancer biology and treatment modalities.
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  46. A15680
    Bilobetin

    PPAR Activator

    Bilobetin acts as a PPARα activator, enhancing lipid metabolism and insulin sensitivity. It effectively reduces blood lipid levels by promoting hepatic lipid uptake and oxidation, while decreasing triglyceride secretion and accumulation in tissues. Additionally, Bilobetin stimulates the phosphorylation and nuclear translocation of PPARα, resulting in increased cAMP levels and PKA activity. This compound is significant for research in metabolic disorders, particularly those related to insulin resistance and lipid regulation.
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  47. A31262
    PT-262

    ROCK Inhibitor

    PT-262 is a selective ROCK inhibitor with an IC50 of approximately 5 μM. This compound induces loss of mitochondrial membrane potential and enhances caspase-3 activation, leading to apoptosis. PT-262 also inhibits phosphorylation of ERK and CDC2 through a p53-independent mechanism, disrupts cytoskeletal dynamics, and impairs cell migration. Its efficacy in promoting anti-cancer activity makes PT-262 a valuable reagent for cancer research.
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  48. A31505
    Y-27632 hydrochloride hydrate

    Selective ROCK Inhibitor

    Y-27632 hydrochloride hydrate is a selective inhibitor of Rho-associated protein kinases (ROCK-I and ROCK-II), exhibiting ATP-competitive activity with IC50 values of 220 nM and 300 nM, respectively. This compound has been shown to reduce Doxorubicin-induced apoptosis in human cardiac stem cells and suppress apoptosis in dissociation-induced murine prostate stem/progenitor cells. Additionally, Y-27632 hydrochloride hydrate enhances the differentiation of human induced pluripotent stem cells (hIPSCs) towards a mesendodermal lineage by modulating epithelial-mesenchymal transition.
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  49. A30007
    8-Bromo-cAMP

    PKA Activator

    8-Bromo-cAMP, a cyclic AMP analog, serves as a potent activator of cyclic AMP-dependent protein kinase (PKA). This compound demonstrates significant anti-proliferative and apoptotic effects in various cancer cell lines, making it a valuable tool for cancer research. Its role in modulating PKA activity provides insights into cellular signaling pathways and the mechanisms of tumorigenesis. 8-Bromo-cAMP is commonly utilized in studies aimed at understanding the therapeutic potential of targeting PKA in cancer treatment.
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  50. A30249
    PKCβ inhibitor 1

    PKCβ Inhibitor

    PKCβ Inhibitor 1 is a highly selective, ATP-competitive inhibitor targeting protein kinase C beta (PKCβ) with IC50 values of 21 nM for PKCβ1 and 5 nM for PKCβ2. This compound demonstrates over 60-fold selectivity for PKCβ2 compared to other PKC isozymes such as PKCα, PKCγ, and PKCε. It is a valuable tool for investigating the roles of PKCβ in various signaling pathways and its implications in diseases such as cancer and diabetes.
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