TGF-β/Smad Inhibitors

TGF-β/Smad inhibitors block transforming growth factor beta (TGF-β) signaling at its receptor kinases or Smad proteins. TGF-β binds a type II receptor kinase, which then phosphorylates the type I receptor, activin receptor-like kinase 5 (ALK5). The activated type I receptor phosphorylates Smad2 and Smad3, which join Smad4 and move into the nucleus to regulate transcription. SB 431542 and A 83-01 inhibit ALK5 together with the related receptors ALK4 and ALK7. RepSox and galunisertib also target the TGF-β type I receptor, while SIS3 blocks Smad3 downstream. LDN193189 instead inhibits ALK2 and ALK3, type I receptors for bone morphogenetic proteins.

Items 1-25 of 151

  • A 83-01
    Cat. No.
    A12358

    A 83-01

    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

    1 mg
    $35.00
    5 mg
    $45.00
    All 7 sizes
  • SB 431542
    Cat. No.
    A10826

    SB 431542

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

    5 mg
    $45.00
    10 mg
    $75.00
    All 6 sizes
  • LY2109761
    Cat. No.
    A11133

    LY2109761

    LY2109761, a novel transforming growth factor β receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis

    2 mg
    $30.00
    5 mg
    $55.00
    All 8 sizes
  • Galunisertib
    Cat. No.
    A11017

    Galunisertib (LY2157299)

    Synonyms: LY-2157299

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

    5 mg
    $25.00
    10 mg
    $35.00
    All 9 sizes
  • LDN193189
    Cat. No.
    A11205

    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.

    2 mg
    $35.00
    5 mg
    $60.00
    All 8 sizes
  • RepSox
    Cat. No.
    A11762

    RepSox (SJN 2511)

    Synonyms: E-616452; SJN 2511; ALK 5 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).

    1 mg
    $25.00
    2 mg
    $35.00
    All 9 sizes
  • LDN193189 HCl
    Cat. No.
    A11478

    LDN193189 HCl

    Synonyms: LDN 193189

    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.

    1 mg
    $30.00
    2 mg
    $45.00
    All 8 sizes
  • Vactosertib
    Cat. No.
    A14213

    Vactosertib (EW-7197)

    Synonyms: EW7197

    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

    2 mg
    $30.00
    5 mg
    $55.00
    All 10 sizes
  • SIS3
    Cat. No.
    A16065

    SIS3

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

    1 mg
    $30.00
    2 mg
    $45.00
    All 9 sizes
  • Pirfenidone
    Cat. No.
    A16209

    Pirfenidone

    Synonyms: AMR69

    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.

    25 mg
    $25.00
    50 mg
    $30.00
    All 8 sizes
  • GW788388
    Cat. No.
    A11083

    GW788388

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

    5 mg
    $30.00
    10 mg
    $55.00
    All 7 sizes
  • DMH-1
    Cat. No.
    A12820

    DMH-1

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

    5 mg
    $45.00
    10 mg
    $75.00
    All 7 sizes
  • ITD-1
    Cat. No.
    A12924

    ITD-1

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

    2 mg
    $25.00
    5 mg
    $45.00
    All 7 sizes
  • Hesperetin
    Cat. No.
    A10449

    Hesperetin

    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.

    5 mg
    $20.00
    10 mg
    $30.00
    All 6 sizes
  • SB 525334
    Cat. No.
    A10827

    SB 525334

    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

    5 mg
    $25.00
    10 mg
    $45.00
    All 7 sizes
  • SB-505124
    Cat. No.
    A11157

    SB-505124

    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).

    1 mg
    $25.00
    2 mg
    $40.00
    All 9 sizes
  • Kartogenin
    Cat. No.
    A12926

    Kartogenin

    Kartogenin potently induces differentiation of human mesenchymal stem cells into chondrocytes

    2 mg
    $25.00
    5 mg
    $40.00
    All 7 sizes
  • LY364947
    Cat. No.
    A13446

    LY364947

    Synonyms: HTS 466284 ,TGF-β RI Kinase Inhibitor

    LY364947 is a diheteroaryl-substituted pyrazole compound used as a selective, ATP-competitive inhibitor of TGF-βRI (TGF-β Receptor I kinase).

    5 mg
    $50.00
    10 mg
    $55.00
    All 8 sizes
  • SD-208
    Cat. No.
    A14066

    SD-208

    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.

    1 mg
    $25.00
    2 mg
    $40.00
    All 8 sizes
  • ML347
    Cat. No.
    A14298

    ML347

    Synonyms: ML 347,ML-347

    ML347 is a selective BMP receptor inhibitor .

    2 mg
    $25.00
    5 mg
    $45.00
    All 7 sizes
  • K02288
    Cat. No.
    A14311

    K02288

    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.

    2 mg
    $25.00
    5 mg
    $45.00
    All 7 sizes
  • A 77-01
    Cat. No.
    A14436

    A 77-01

    A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.

    1 mg
    $35.00
    5 mg
    $90.00
    All 7 sizes
  • Alantolactone
    Cat. No.
    A14810

    Alantolactone

    Alantolactone, an allergenic sesquiterpene lactone, has recently been found to have significant antitumor effects on malignant tumor cells.

    5 mg
    $45.00
    10 mg
    $60.00
    All 6 sizes

Items 1-25 of 151

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