TGF-β/Smad Inhibitors

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  1. 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.
  2. 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 .
  3. 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
  4. TGF-βR Inhibitor

    LY2157299 is an orally active transforming growth factor beta receptor (TGF-βR) kinase inhibitor.
  5. 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).
  6. 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
  7. 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).
  8. 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.
  9. 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.
  10. 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).
  11. 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
  12. ALK2 inhibitor

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

    LDN-212854 is an ALK2-Biased BMP Type I Receptor Kinase Inhibitor.
  14. TGF-β inhibitor

    ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells.
  15. Smad inhibitor

    Kartogenin potently induces differentiation of human mesenchymal stem cells into chondrocytes
  16. 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).
  17. 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.
  18. TGF-beta receptor inhibitor

  19. 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
  20. BMP receptor inhibitor

    ML347 is a selective BMP receptor inhibitor .
  21. 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.
  22. 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.
  23. Alantolactone, an allergenic sesquiterpene lactone, has recently been found to have significant antitumor effects on malignant tumor cells.
  24. TGF-β Receptors Inhibitor

    SB-505124 hydrochloride is an inhibitor of ALK.
  25. Smad3 inhibitor

    SIS3 is a novel specific inhibitor of Smad3. It has effect on transforming growth factor-beta1-induced extracellular matrix expression.
  26. 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.
  27. ALK2 inhibitor

    LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM.
  28. ALK5 inhibitor

    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
  29. Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
  30. 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.
  31. TGF-beta agonist

    SRI-011381 hydrochloride is a TGF-beta signaling agonist.
  32. Cetrimonium bromide is an amine based cationic quaternary surfactant, is one of the components of the topical antiseptic Cetrimide.
  33. 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.
  34. TGFβRI inhibitor

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

    TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively.
  36. BMP activator

    SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.
  37. EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
  38. BMP type I receptor inhibitor

    LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50??500 nM).
  39. BMP signaling inhibitor

    LDN193189 HCl (DM-3189) is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β.
  40. BMP4 signaling agonist

    BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9.

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