TGF-β / Smad

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  1. LY2157299

    Catalog No. A11017
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    TGF-βR Inhibitor
    LY2157299 is an orally active transforming growth factor beta receptor (TGF-βR) kinase inhibitor. Learn More
  2. SB 431542

    Catalog No. A10826
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    TGF-beta/Smad inhibitor
    SB 431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7 . Learn More
  3. GW788388

    Catalog No. A11083
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    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). Learn More
  4. SB-505124

    Catalog No. A11157
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    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). Learn More
  5. LDN193189

    Catalog No. A11205
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    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. Learn More
  6. SB 525334

    Catalog No. A10827
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    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 Learn More
  7. LY2109761

    Catalog No. A11133
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    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 Learn More
  8. Hesperetin

    Catalog No. A10449
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    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. Learn More
  9. RepSox (SJN 2511)

    Catalog No. A11762
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    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). Learn More
  10. A 83-01

    Catalog No. A12358
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    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 Learn More
  11. DMH-1

    Catalog No. A12820
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    ALK2 inhibitor
    DMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM). Learn More
  12. LDN-212854

    Catalog No. A12821
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    BMP receptor inhibitor
    LDN-212854 is an ALK2-Biased BMP Type I Receptor Kinase Inhibitor. Learn More
  13. ITD-1

    Catalog No. A12924
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    TGF-β inhibitor
    ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells. Learn More
  14. Kartogenin

    Catalog No. A12926
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    Smad inhibitor
    Kartogenin potently induces differentiation of human mesenchymal stem cells into chondrocytes Learn More
  15. F9995-0144

    Catalog No. A14162
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    TGF-beta receptor inhibitor
  16. EW-7197

    Catalog No. A14213
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    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 Learn More
  17. LDN193189 HCl

    Catalog No. A11478
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    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. Learn More
  18. ML347

    Catalog No. A14298
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    BMP receptor inhibitor
    ML347 is a selective BMP receptor inhibitor . Learn More
  19. K02288

    Catalog No. A14311
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    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. Learn More
  20. A 77-01

    Catalog No. A14436
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    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. Learn More
  21. LY364947

    Catalog No. A13446
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    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). Learn More
  22. Alantolactone

    Catalog No. A14810
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    Alantolactone, an allergenic sesquiterpene lactone, has recently been found to have significant antitumor effects on malignant tumor cells. Learn More
  23. NG25

    Catalog No. A15185
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    TAK1/MAP4K2 inhibitor
    NG25, a TAK1 inhibitor, inhibited the activation of IKK by TLR7 and TLR9 agonists and prevented the secretion of type 1 IFNs induced by these ligands in Gen2.2 cells. Learn More
  24. SB-505124 HCl

    Catalog No. A15232
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    TGF-β Receptors Inhibitor
    SB-505124 hydrochloride is an inhibitor of activin receptor-like kinases (ALKs). Learn More
  25. SD-208

    Catalog No. A14066
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    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. Learn More
  26. SIS3

    Catalog No. A16065
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    Smad3 inhibitor
    SIS3 is a novel specific inhibitor of Smad3. It has effect on transforming growth factor-beta1-induced extracellular matrix expression. Learn More
  27. (+)-ITD 1

    Catalog No. A16073
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    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. Learn More
  28. LDN-214117

    Catalog No. A16096
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    ALK2 inhibitor
    LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM. Learn More
  29. R-268712

    Catalog No. A16207
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    ALK5 inhibitor
    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM. Learn More
  30. Chebulinic acid

    Catalog No. A16208
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    Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity. Learn More
  31. Pirfenidone

    Catalog No. A16209
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    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. Learn More
  32. SRI-011381 hydrochloride

    Catalog No. A16210
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    TGF-beta agonist
    SRI-011381 hydrochloride is a TGF-beta signaling agonist. Learn More
  33. LY 3200882

    Catalog No. A16816
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    TGFβRI inhibitor
    LY 3200882 is a potent, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). It potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion. Learn More
    • New

    BIBF0775

    Catalog No. A17230
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    TGFβRI inhibitor
    BIBF0775 is an inhibitor of the transforming growth factor β receptor I (TGFβRI). Learn More
  34. PKC 412 (Midostaurin)

    Catalog No. A12650
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    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. Learn More
  35. GO6983

    Catalog No. A13790
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    PKC inhibitor
    GO6983 is a potent protein kinase C (PKC) inhibitor. It reduces polymorphonuclear leukocyte adherence and infiltration following myocardial ischemia/reperfusion injury. Learn More
  36. Ro 31-8220

    Catalog No. A13514
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    PKC inhibitor
    Ro 31-8220 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%. Learn More
  37. 12-O-tetradecanoyl phorbol-13-acetate

    Catalog No. A14616
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    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. Learn More
  38. PKC (19-36)

    Catalog No. A14871
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    PKC inhibitor
    PKC (19-36), pseudosubstrate peptide inhibitor of protein kinase C (IC50 = 0.18 uM). Learn More
  39. (-)-Indolactam V

    Catalog No. A13043
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    PKC activator
    (-)-Indolactam V is a protein kinase C activator, which strongly directs human ES cell-derived definitive endoderm into pancreatic endoderm. Learn More
  40. PKC-IN-1

    Catalog No. A16212
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    PKC inhibitor
    PKC-IN-1 is a poent PKC beta II inhibitor with Ki of 14.9 nM; compound example H6 from patent WO 2008096260 A1. Learn More
  41. NSC305787

    Catalog No. A16213
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    PKC inhibitor
    NSC305787 is a small molecule inhibitor of PKC, with IC50 of 8.3 uM, 9.4 uM, 55 uM for PKC phosphorylation of recombinant ezrin, of moesin, and of radixin. Learn More
  42. LY317615 (Enzastaurin)

    Catalog No. A10356
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    PKCβ inhibitor
    LY317615 (Enzastaurin) is a potent and selective inhibitor of PKCβ with antiproliferative activity (IC50= ~6 nM). Learn More
  43. Daphnetin

    Catalog No. A10286
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    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. Learn More
  44. Quercetin (Sophoretin)

    Catalog No. A10766
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    MAO-B inhibitor
    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C. Learn More
  45. Chelerythrine Chloride

    Catalog No. A10196
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    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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  46. Myricitrin (Myricitrine)

    Catalog No. A10616
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    Myricitrin is the 3-O-rhamnoside of myricetin. Myricitrin is used by several beetle species in their communication system. Learn More
  47. Bryostatin 1

    Catalog No. A10261
    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. Learn More
  48. Sotrastaurin (AEB071)

    Catalog No. A11554
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    PKC inhibitor
    Sotrastaurin is a protein kinase C inhibitor for the prevention of transplant rejection and treatment of psoriasis. Learn More
  49. Staurosporine

    Catalog No. A10864
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    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. Learn More

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