TGF-β / Smad Inhibitors

Catalog No.Inhibitor Name ALK1ALK2ALK3ALK4TGFβRI/ALK5ALK6ALK7TGFβRIITGF-βSmad3Other
A10826SB431542
**
A11205LDN-193189
****
***
A11017Galunisertib
**
A11133LY2109761
***
*
A10827SB525334
***
A11157SB505124
**
**
A11083GW788388
***
A13446LY364947
**
*
RIPK2,CK1δ,MLK-7K
A11762RepSox
****
A11478LDN-193189 HCl
****
***
A14311K02288
****
****
***
*
*
****
A16096LDN-214117
***
A14066SD-208
**
A14213EW-7197
***
****
A14298ML347
**
***
*
*
A12821LDN-212854
****
****
**
*
*
A12820DMH1
**
A16209Pirfenidone
A10449Hesperetin
Histamine receptor
A12358A 83-01
***
**
****
A12924ITD 1
*
A14436A 77-01
***
A16065SIS3
A16207R-268712
****

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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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. 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
  3. 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
  4. 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
  5. 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. (+)-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
  11. 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
  12. 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
  13. 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
  14. 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
  15. SRI-011381 hydrochloride

    Catalog No. A16210
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    TGF-beta agonist
    SRI-011381 hydrochloride is a TGF-beta signaling agonist. Learn More
  16. ML347

    Catalog No. A14298
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    BMP receptor inhibitor
    ML347 is a selective BMP receptor inhibitor . Learn More
  17. LDN193189 HCl

    Catalog No. A11478
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    LDN193189 HCl is the hydrochloride salt of LDN193189. Learn More
  18. 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
  19. 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
  20. 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
  21. 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
  22. 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
  23. 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
  24. 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
  25. 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
  26. 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
  27. 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
  28. 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
  29. 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
  30. Kartogenin

    Catalog No. A12926
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    Smad inhibitor
    Kartogenin potently induces differentiation of human mesenchymal stem cells into chondrocytes Learn More
  31. 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
  32. 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

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