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Home >> Signaling Pathways >> TGF-β / Smad Signaling

TGF-β / Smad Signaling

Transforming growth factor-beta (TGF-beta) is a multifunctional cytokine that regulates proliferation, migration, differentiation, and survival of many different cell types. Deletion or mutation of different members of the TGF-β family have been shown to cause vascular remodeling defect and absence of mural cell formation, leading to embryonic lethality or severe vascular disorders. TGF-β induces smooth muscle differentiation via Notch or SMAD2 and SMAD3 signaling in ES cells or in a neural crest stem cell line. TGF-β binds to TGF-βRI and to induce phosphorylation of SMAD2/3, thereby inhibiting proliferation, tube formation, and migration of endothelial cells (ECs).

TGF-β is a pluripotent cytokine with dual tumour-suppressive and tumour-promoting effects. TGF-β induces the epithelial-to-mesenchymal transition (EMT) leading to increased cell plasticity at the onset of cancer cell invasion and metastasis.

Targets for  TGF-β / Smad Signaling

Products for  TGF-β / Smad Signaling

  1. Cat.No. Product Name Information
  2. GC10716 Netarsudil (AR-13324) ROCK inhibitor Netarsudil (AR-13324) Chemical Structure
  3. GC13514 NG25 An inhibitor of MAP4K2 and TAK1 NG25 Chemical Structure
  4. GC25669 Nilotinib hydrochloride

    AMN-107 HCl

     Nilotinib hydrochloride (AMN-107) is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Nilotinib hydrochloride Chemical Structure
  5. GC14075 Nocodazole

    NSC 238159, Oncodazole, R 17934

     Nocodazole is an anti-mitotic drug and a rapid and reversible microtubule polymerization inhibitor. It inhibits Abl, Abl (E255K), and Abl (T315I) in cell-free assays with IC50 values of 0.21μM, 0.53μM, and 0.64μM, respectively. Nocodazole Chemical Structure
  6. GC60274 O-Desmethyl Midostaurin

    CGP62221; O-Desmethyl PKC412

     O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo. Midostaurin is a multi-targeted protein kinase inhibitor?with?IC50?ranging from 22-500 nM. O-Desmethyl Midostaurin Chemical Structure
  7. GC36807 ON 146040 ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM). ON 146040 Chemical Structure
  8. GN10378 Oxymatrine

    Matrine 1oxide

     Oxymatrine Chemical Structure
  9. GC36833 p32 Inhibitor M36

    M36

     p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1. p32 Inhibitor M36 Chemical Structure
  10. GC12637 PD 180970 P210bcr/abl tyrosine kinase inhibitor PD 180970 Chemical Structure
  11. GC72924 PD173952 PD173952 is a tyrosine kinases inhibitor with IC50s of 0.3, 1.7 and 6.6 nM against Lyn, Abl and Csk, respectively. PD173952 Chemical Structure
  12. GC13592 PD173955 Dual Src/Abl kinase inhibitor, ATP-competitive, PD173955 Chemical Structure
  13. GC33901 Pentanoic acid Pentanoic acid Chemical Structure
  14. GC61585 Pep2m, myristoylated TFA

    Myr-Pep2m TFA

     Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide. Pep2m, myristoylated TFA Chemical Structure
  15. GC14767 PF-00562271

    PF-562271;PF00562271;PF62271

     PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively. PF-00562271 Chemical Structure
  16. GC14407 PF-431396 Pyk2 and FAK inhibitor PF-431396 Chemical Structure
  17. GC15380 PF-562271

    PF562271;PF 562271

     PF-562271 is a potent small-molecule inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (Pyk2) with a IC50 of 1.5 and 14nmol/L, respectively. PF-562271 Chemical Structure
  18. GC10810 PF-562271 HCl

    PF562271 HCl;PF 562271 HCl

     PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively. PF-562271 HCl Chemical Structure
  19. GC17352 Phorbol 12,13-dibutyrate

    PDBu

     Protein kinase C activator Phorbol 12,13-dibutyrate Chemical Structure
  20. GC73968 Pim-1 kinase inhibitor 8 Pim-1 kinase inhibitor 8 (compound 12) is a potent inhibitor of Pim-1 kinase with an IC50 of 14.3 nM. Pim-1 kinase inhibitor 8 Chemical Structure
  21. GC12790 Pirfenidone

    AMR 69

     Pirfenidone (AMR69) is an orally active antifibrotic drug that attenuates the production of chemokines CCL2 and CCL12 in fibrocytes . Pirfenidone Chemical Structure
  22. GC40197 Pirfenidone-d5 Pirfenidone-d5 is intended for use as an internal standard for the quantification of pirfenidone by GC- or LC-MS. Pirfenidone-d5 Chemical Structure
  23. GC15471 PKC β pseudosubstrate Selective cell-permeable peptide inhibitor of protein kinase C PKC β pseudosubstrate Chemical Structure
  24. GC10404 PKC ζ pseudosubstrate PKC ζ pseudosubstrate is a selective cell-permeable inhibitor of PKC. PKC ζ pseudosubstrate Chemical Structure
  25. GC11671 PKC fragment (530-558) Potent activator of protein kinase C PKC fragment (530-558) Chemical Structure
  26. GC61995 PKCβ inhibitor 1

    Protein Kinase Cβ Inhibitor

     PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε). PKCβ inhibitor 1 Chemical Structure
  27. GC44655 PKCε Inhibitor Peptide

    Protein Kinase Cɛ Inhibitor Peptide，ɛV1-2

     PKCε Inhibitor Peptide, also called εV1-2, is a protein kinase C ε (PKCε)-derived peptide, act as a selective PKCε inhibitor, inhibits the translocation of PKCε . PKCε Inhibitor Peptide Chemical Structure
  28. GC74417 PKCθ pseudosubstrate peptide inhibitor,myristoylated TFA PKCθ pseudosubstrate peptide inhibitor, myristoylated TFA is a synthetic peptide that can be used to study the mechanism of action of PKCθ. PKCθ pseudosubstrate peptide inhibitor,myristoylated TFA Chemical Structure
  29. GC31711 PKC-IN-1 PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively. PKC-IN-1 Chemical Structure
  30. GC65126 PKC-iota inhibitor 1 PKC-iota inhibitor 1 (compound 19) is a protein kinase C-iota (PKC-ι ?) inhibitor with an IC50 value of 0.34 μM. PKC-iota inhibitor 1 Chemical Structure
  31. GC30200 PKC-theta inhibitor PKC-theta inhibitor is a selective PKC-θinhibitor, with an IC50 of 12 nM. PKC-theta inhibitor Chemical Structure
  32. GC70591 PKC-theta inhibitor 1 PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. PKC-theta inhibitor 1 Chemical Structure
  33. GC67686 PKCiota-IN-2 formic PKCiota-IN-2 formic Chemical Structure
  34. GC14396 Ponatinib (AP24534)

    AP 24534

     Ponatinib (AP24534) (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively. Ponatinib (AP24534) Chemical Structure
  35. GC45828 Ponatinib-d8 An internal standard for the quantification of ponatinib Ponatinib-d8 Chemical Structure
  36. GC68339 Ponsegromab

    PF 06946860

     Ponsegromab Chemical Structure
  37. GC12779 PPY A Abl kinases inhibitor PPY A Chemical Structure
  38. GC36974 Procyanidin A1 Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca2+ influx from an internal store in RBL-213 cells. Procyanidin A1 Chemical Structure
  39. GC44729 Prostratin

    13-O-Acetylphorbol

     An HIV reactivator Prostratin Chemical Structure
  40. GC73444 PROTAC BCR-ABL Degrader-1 PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoetl linker. PROTAC BCR-ABL Degrader-1 Chemical Structure
  41. GC37014 Protein Kinase C 19-31

    PKC (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 19-31 Chemical Structure
  42. GC37015 Protein Kinase C 19-36 Protein Kinase C 19-36 is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM. Protein Kinase C 19-36 Chemical Structure
  43. GC66006 Protein kinase inhibitor H-7 Protein kinase inhibitor H-7 is a potent inhibitor of protein kinase C (PKC) and cyclic nucleotide dependent protein kinase, with a Ki of 6 μM for PKC. Protein kinase inhibitor H-7 Chemical Structure
  44. GC73424 PRT062607 acetate

    P505-15 acetate; PRT-2607 acetate; BIIB-057 acetate

     PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate Chemical Structure
  45. GC72880 PS432 PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 Chemical Structure
  46. GC11803 Pseudo RACK1 Activator of protein kinase C Pseudo RACK1 Chemical Structure
  47. GC69776 PT-262

    PT-262 is an effective ROCK inhibitor with an IC50 value of approximately 5 μM. PT-262 induces loss of mitochondrial membrane potential and increases activation of caspase-3 and cell apoptosis. PT-262 inhibits phosphorylation of ERK and CDC2 through a p53-independent pathway. PT-262 blocks cellular cytoskeleton function and cell migration. PT-262 has anti-cancer activity.

     PT-262 Chemical Structure
  48. GC74116 Pyk2-IN-2 Pyk2-IN-2 (compound 13j) is an inhibitor of Pyk2 with an IC50 of FAK kinase of 0.608 μM. Pyk2-IN-2 Chemical Structure
  49. GC14583 R 59-022

    Diacylglycerol Kinase Inhibitor I

     Diacylglycerol (DAG) kinase inhibitor R 59-022 Chemical Structure
  50. GC69792 R 59-022 hydrochloride

    DKGI-I hydrochloride; Diacylglycerol kinase inhibitor I hydrochloride

    R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 μM). R 59-022 hydrochloride inhibits OAG phosphorylation to OAPA. It is also a 5-HT receptor antagonist that can activate protein kinase C (PKC). R 59-022 enhances the production of thromboxane in platelets induced by thrombin and inhibits phosphatidic acid production in neutrophils.

     R 59-022 hydrochloride Chemical Structure
  51. GC32840 R-268712 R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 Chemical Structure
  52. GC18246 R-59-949

    Diacylglycerol Kinase Inhibitor II, DKGI-II

    R-59-949 is an inhibitor of diacylglycerol kinase α (DGK-α) with an IC50 value of 300 nM in isolated platelet plasma membranes using exogenous diacylglycerol as a substrate.

     R-59-949 Chemical Structure
  53. GC11140 Radotinib(IY-5511)

    IY-5511

     Bcr-Abl tyrosine kinase inhibitor Radotinib(IY-5511) Chemical Structure
  54. GC16793 RepSox

    E 616452, RepSox, SJN 2511

     RepSox is a potent and selective inhibitor of transforming growth factor-β receptor I/activin-like kinase 5 (TGF-β-RI/ALK5) with an IC50 of 23nM. RepSox inhibits ALK5 autophosphorylation with an IC50 of 4nM. RepSox Chemical Structure
  55. GC33310 Rho-Kinase-IN-1 Rho-Kinase-IN-1 is a Rho kinase (ROCK) inhibitor (Ki values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively) extracted from US20090325960A1, compound 1.008. Rho-Kinase-IN-1 Chemical Structure
  56. GC66050 Rho-Kinase-IN-2 Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington's research. Rho-Kinase-IN-2 Chemical Structure
  57. GC70451 Rho-Kinase-IN-3 Rho-Kinase-IN-3 (compound 12) is a potent and selective Rho kinase (ROCK1) inhibitor with an IC50 value of 8 nM. Rho-Kinase-IN-3 Chemical Structure
  58. GC72976 Rhodblock 6 Rhodblock 6 is a Rho kinase (ROCK) inhibitor that inhibits phospho-MRLC (myosin regulatory light chain) localization. Rhodblock 6 Chemical Structure
  59. GC37534 Ripasudil free base

    K-115 (free base)

     Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively. Ripasudil free base Chemical Structure
  60. GC73201 Risvodetinib

    IkT-148009

     Risvodetinib (IkT-148009) is an oral, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM. Risvodetinib Chemical Structure
  61. GC17322 Ro 31-8220

    Bisindolylmaleimide IX

     pan-PKC inhibitor Ro 31-8220 Chemical Structure
  62. GC17014 Ro 31-8220 Mesylate Pan-PKC inhibitor Ro 31-8220 Mesylate Chemical Structure
  63. GC10029 Ro 31-8220 methanesulfonate

    BIM IX, Ro 318220

     Ro 31-8220 methanesulfonate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 methanesulfonate Chemical Structure
  64. GC13677 Ro 32-0432 hydrochloride protein kinase C inhibitor Ro 32-0432 hydrochloride Chemical Structure
  65. GC37551 ROCK inhibitor-2 ROCK inhibitor-2 is a selective dual ROCK1 and ROCK2 inhibitor with IC50s of 17 nM and 2 nM, respectively. ROCK inhibitor-2 Chemical Structure
  66. GC31952 ROCK-IN-1 ROCK-IN-1 is a potent inhibitor of ROCK, with an IC50 of 1.2 nM for ROCK2. ROCK-IN-1 Chemical Structure
  67. GC66338 ROCK1-IN-1 ROCK1-IN-1 is a ROCK1 inhibitor with a Ki value of 540 nM. ROCK1-IN-1 can be used for the research of hypertension, glaucoma and erectile dysfunction. ROCK1-IN-1 Chemical Structure
  68. GC31883 ROCK2-IN-2 ROCK2-IN-2 is a selective ROCK2 inhibitor extracted from patent US20180093978A1, Compound A-30, has an IC50 of <1 μM. ROCK2-IN-2 Chemical Structure
  69. GC71389 ROCK2-IN-6 hydrochloride ROCK2-IN-6 hydrochloride (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research. ROCK2-IN-6 hydrochloride Chemical Structure
  70. GC10820 Rottlerin

    Mallotoxin, NSC 94525, NSC 56346

     PKC inhibitor Rottlerin Chemical Structure
  71. GC63177 Ruboxistaurin

    LY333531

     Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin Chemical Structure
  72. GC16405 Safingol

    L-threo-Dihydrosphingosine,L-threo-Sphinganine

     PKC and sphingosine kinases inhibitor Safingol Chemical Structure
  73. GC72185 SAMβA TFA SAMβA TFA is conjugated to the cell permeable peptide TAT47-57. SAMβA TFA Chemical Structure
  74. GC63439 Sangivamycin Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers. Sangivamycin Chemical Structure
  75. GC13759 SAR407899 ATP-competitive ROCK inhibitor SAR407899 Chemical Structure
  76. GC16289 SAR407899 hydrochloride ATP-competitive ROCK inhibitor SAR407899 hydrochloride Chemical Structure
  77. GC15197 Saracatinib (AZD0530)

    AZD 0530

     Saracatinib (AZD0530) (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib (AZD0530) shows high selectivity over other tyrosine kinases. Saracatinib (AZD0530) Chemical Structure
  78. GC11022 SB 218078 checkpoint kinase 1 (Chk1) inhibitor SB 218078 Chemical Structure
  79. GC11545 SB 431542 SB-431542, a small molecule inhibitor of the type I TGF-β receptor, blocks intracellular mediators of TGF-1 signaling, which leads to decreased TGF-β1–mediated proliferation, cytokines and collagen expression. SB 431542 Chemical Structure
  80. GC15170 SB 772077B dihydrochloride Rho-kinase (ROCK) inhibitor SB 772077B dihydrochloride Chemical Structure
  81. GC10421 SB-505124 hydrochloride

    SB 505124 hydrochloride;SB505124 hydrochloride

     Inhibitor of receptors ALK4, ALK5, and ALK7 SB-505124 hydrochloride Chemical Structure
  82. GC13769 SB505124 ALK4/ALK5/ALK7 inhibitor SB505124 Chemical Structure
  83. GC14349 SB525334

    TGF-β RI Kinase Inhibitor VIII

     (TGF-beta1) receptor inhibitor SB525334 Chemical Structure
  84. GC13320 SC-10 Protein kinase C activator SC-10 Chemical Structure
  85. GC18055 SC-9

    NCM 119

     protein kinase C activator SC-9 Chemical Structure
  86. GC13904 SD-208

    TGF-β RI Kinase Inhibitor V

     A potent, selective inhibitor of TGF-βRI SD-208 Chemical Structure
  87. GC74617 SHR-1701

    Retlirafusp alfa

     SHR-1701 (Retlirafusp alfa) is a bifunctional fusion protein targeting PD-L1 and TGF-β for cancer research. SHR-1701 Chemical Structure
  88. GC73377 SIAIS100 TFA SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 TFA Chemical Structure
  89. GC17191 SIS3 HCl SIS3 HCl is a Smad3 inhibitor that inhibits the phosphorylation of Smad3 with an IC50 of 3 μM. SIS3 HCl Chemical Structure
  90. GC69903 SJ000063181

    SJ000063181 is an effective BMP signal activator with an EC50 ≤1 µM. It can be used as a chemical probe to explore BMP signaling because it can penetrate zebrafish embryos.

     SJ000063181 Chemical Structure
  91. GC32788 SJ000291942 A BMP signaling activator SJ000291942 Chemical Structure
  92. GC19447 SM 16

    SM 16 is a ALK5/ALK4 kinase inhibitor

     SM 16 Chemical Structure
  93. GC44903 SMAD3 Inhibitor, SIS3 SMAD3 Inhibitor, SIS3 is a potent and selective inhibitor of Smad3 phosphorylation. SMAD3 Inhibitor, SIS3 Chemical Structure
  94. GC65592 SNIPER(ABL)-020 SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein. SNIPER(ABL)-020 Chemical Structure
  95. GC15520 Sotrastaurin (AEB071)

    AEB 071;AEB-071

     Sotrastaurin (AEB071) (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively. Sotrastaurin (AEB071) Chemical Structure
  96. GC10722 SR-3677 Rho Kinase (ROCK-II) inhibitor SR-3677 Chemical Structure
  97. GC19338 SRI-011381 hydrochloride An oral bioavailabile TGF-beta signaling agonist SRI-011381 hydrochloride Chemical Structure
  98. GC72410 Stamulumab Stamulumab (MYO-029) is a recombinant human IgG1λ antibody that binds to myostatin and neutralizes its activity by preventing binding to its endogenous high-affinity receptor ActRIIB. Stamulumab Chemical Structure
  99. GC15299 Staurosporine(CGP 41251)

    Stsp

     Staurosporin, a small kinase inhibitor, is an alkaloid derived from the bacterium Streptomyces staurosporeus. Staurosporine(CGP 41251) Chemical Structure
  100. GC69981 SY-LB-35

    SY-LB-35 is an effective bone morphogenetic protein (BMP) receptor agonist. It can stimulate C2C12 cells to significantly increase cell number and cell vitality, causing the cell cycle to transition into S phase and G2/M phase. SY-LB-35 stimulates typical Smad and atypical PI3K/Akt, ERK, p38, and JNK intracellular signaling pathways.

     SY-LB-35 Chemical Structure
  101. GC16821 TAE226(NVP-TAE226)

    TAE 226;TAE-226

     TAE226(NVP-TAE226) (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. TAE226(NVP-TAE226) Chemical Structure

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