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.

Products for  TGF-β / Smad Signaling

  1. Cat.No. Product Name Information
  2. GC70166 Z-Arg-SBzl Z-Arg-SBzl  Chemical Structure
  3. GC70110 Vamotinib Vamotinib  Chemical Structure
  4. GC70050 Trabedersen Trabedersen  Chemical Structure
  5. GC69981 SY-LB-35 SY-LB-35  Chemical Structure
  6. GC69903 SJ000063181 SJ000063181  Chemical Structure
  7. GC69792 R 59-022 hydrochloride R 59-022 hydrochloride  Chemical Structure
  8. GC69776 PT-262 PT-262  Chemical Structure
  9. GN10534 Asiaticoside Asiaticoside  Chemical Structure
  10. GN10463 Chelerythrine Chelerythrine  Chemical Structure
  11. GN10378 Oxymatrine Oxymatrine  Chemical Structure
  12. GN10336 Daphnetin Daphnetin  Chemical Structure
  13. GN10444 12-O-tetradecanoyl phorbol-13-acetate

    A PKC activator

    12-O-tetradecanoyl phorbol-13-acetate  Chemical Structure
  14. GC13904 SD-208 A potent, selective inhibitor of TGF-βRI SD-208  Chemical Structure
  15. GC10421 SB-505124 hydrochloride Inhibitor of receptors ALK4, ALK5, and ALK7 SB-505124 hydrochloride  Chemical Structure
  16. GC16793 RepSox A selective inhibitor of ALK5 RepSox  Chemical Structure
  17. GC13514 NG25 An inhibitor of MAP4K2 and TAK1 NG25  Chemical Structure
  18. GC14931 LDN193189 Hydrochloride An inhibitor of BMP receptors ALK1, ALK2, ALK3, and ALK6 LDN193189 Hydrochloride  Chemical Structure
  19. GC13065 Chelerythrine Chloride Potent inhibitor of PKC and Bcl-xL Chelerythrine Chloride  Chemical Structure
  20. GC14650 CGP60474 A CDK inhibitor CGP60474  Chemical Structure
  21. GC10166 A 83-01 A TGF-β type I receptor inhibitor A 83-01  Chemical Structure
  22. GC13927 A 77-01 A potent ALK5 inhibitor A 77-01  Chemical Structure
  23. GC15299 Staurosporine(CGP 41251) A potent inhibitor of protein kinase C Staurosporine(CGP 41251)  Chemical Structure
  24. GC14049 (-)-Epigallocatechin gallate (EGCG) A phenol with diverse biological activities (-)-Epigallocatechin gallate (EGCG)  Chemical Structure
  25. GC26065 WAY-354831 WAY-354831 exhibits antibacterial activity. WAY-354831  Chemical Structure
  26. GC26055 WAY-301398 WAY-301398 (6-methoxynaphthalene) can bind to protein kinase C (PKC). WAY-301398  Chemical Structure
  27. GC26000 TP0427736 HCl TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. TP0427736 HCl  Chemical Structure
  28. GC25669 Nilotinib hydrochloride 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
  29. GC25662 N-Desmethyltamoxifen N-Desmethyltamoxifen, the major metabolite of Tamoxifen in humans and a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen, also is a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. N-Desmethyltamoxifen  Chemical Structure
  30. GC25482 GSK269962A HCl GSK269962A HCl (GSK269962B, GSK269962) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively. GSK269962A HCl  Chemical Structure
  31. GC68339 Ponsegromab Ponsegromab  Chemical Structure
  32. GC68333 Disitertide diammonium Disitertide diammonium  Chemical Structure
  33. GC67686 PKCiota-IN-2 formic PKCiota-IN-2 formic  Chemical Structure
  34. 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
  35. 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
  36. 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
  37. 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
  38. GC65585 Mongersen Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen  Chemical Structure
  39. GC65539 Fresolimumab Fresolimumab (GC1008) is a high-affinity fully human monoclonal antibody that neutralizes the active form of human TGFβ1, TGFβ2, and TGFβ3. Fresolimumab  Chemical Structure
  40. GC65329 EW-7195 EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung. EW-7195  Chemical Structure
  41. GC65294 ALK2-IN-2 ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3. ALK2-IN-2  Chemical Structure
  42. 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
  43. GC64815 Aurothiomalate sodium Aurothiomalate sodium is a potent and selective oncogenic PKCι signaling inhibitor. Aurothiomalate sodium  Chemical Structure
  44. GC64462 Asciminib hydrochloride Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM. Asciminib hydrochloride  Chemical Structure
  45. GC64326 Hydrochlorothiazid-d2 Hydrochlorothiazid-d2  Chemical Structure
  46. GC64263 Kobophenol A Kobophenol A, an oligomeric stilbene, blocks the interaction between the ACE2 receptor and S1-RBD with an IC50 of 1.81 μM and inhibits SARS-CoV-2 viral infection in cells with an EC50 of 71.6 μM. Kobophenol A  Chemical Structure
  47. GC63829 A 83-01 sodium A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively. A 83-01 sodium  Chemical Structure
  48. GC63778 Myelin Basic Protein TFA Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein TFA  Chemical Structure
  49. 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
  50. GC63177 Ruboxistaurin Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin  Chemical Structure
  51. GC62868 BIO-013077-01 BIO-013077-01 is a pyrazole TGF-β inhibitor. BIO-013077-01  Chemical Structure
  52. GC49269 Myr-ZIP A PKMζ inhibitor Myr-ZIP  Chemical Structure
  53. GC62612 CC-90005 CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005  Chemical Structure
  54. GC62478 ζ-Stat ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro. ζ-Stat  Chemical Structure
  55. GC62146 XST-14 XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects. XST-14  Chemical Structure
  56. GC61776 Ingenol 3,20-dibenzoate Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate  Chemical Structure
  57. GC61585 Pep2m, myristoylated TFA Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide. Pep2m, myristoylated TFA  Chemical Structure
  58. GC50704 CRT 0066854 hydrochloride CRT 0066854 hydrochloride is a potent and selective atypical PKCs inhibitor. CRT 0066854 hydrochloride  Chemical Structure
  59. GC60782 Disitertide TFA Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer. Disitertide TFA  Chemical Structure
  60. GC60274 O-Desmethyl Midostaurin 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
  61. GC60210 Isosaponarin Isosaponarin is a flavone glycoside isolated from wasabi leaves. Isosaponarin  Chemical Structure
  62. GC60037 A-3 hydrochloride A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. A-3 hydrochloride  Chemical Structure
  63. GC39398 LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier. LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)  Chemical Structure
  64. GC50593 BMP signaling agonist sb4

    Potent BMP4 agonist

    BMP signaling agonist sb4  Chemical Structure
  65. GC50589 AZ 12799734 Potent TGF-βRI inhibitor AZ 12799734  Chemical Structure
  66. GC50317 IN 1130 Potent and selective inhibitor of TGF-βRI IN 1130  Chemical Structure
  67. GC38931 N-Desmethyltamoxifen hydrochloride N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. N-Desmethyltamoxifen hydrochloride  Chemical Structure
  68. GC38898 CCG-222740 CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis. CCG-222740  Chemical Structure
  69. GC38791 GSK-25 GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25  Chemical Structure
  70. GC45828 Ponatinib-d8 An internal standard for the quantification of ponatinib Ponatinib-d8  Chemical Structure
  71. GC38482 Desmethylglycitein Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities.Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes. Desmethylglycitein  Chemical Structure
  72. GC38388 DCPLA-ME DCPLA-ME, the methyl ester form of DCPLA, is a potent PKCε activator for use in the treatment of neurodegenerative diseases. DCPLA-ME  Chemical Structure
  73. GC38186 Daphnoretin A coumarin with diverse biological activities Daphnoretin  Chemical Structure
  74. GC38085 Decursinol angelate Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities. Decursinol angelate  Chemical Structure
  75. GC45414 CRT0066854   CRT0066854  Chemical Structure
  76. GC37947 Y-33075 Y-33075 is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM. Y-33075  Chemical Structure
  77. GC37880 Vactosertib Hydrochloride Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect. Vactosertib Hydrochloride  Chemical Structure
  78. 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
  79. GC37534 Ripasudil 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
  80. 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
  81. GC37014 Protein Kinase C 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
  82. 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
  83. GC36833 p32 Inhibitor 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
  84. 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
  85. GC36433 LDN193189 Tetrahydrochloride A selective BMP type I receptor inhibitor LDN193189 Tetrahydrochloride  Chemical Structure
  86. GC36282 Hypocrellin A Hypocrellin A, a naturally occurring PKC inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities. Hypocrellin A  Chemical Structure
  87. GC36208 H-1152 dihydrochloride H-1152 dihydrochloride is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2. H-1152 dihydrochloride  Chemical Structure
  88. GC36207 H-1152 H-1152 is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2. H-1152  Chemical Structure
  89. GC36167 GMB-475 GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein. GMB-475  Chemical Structure
  90. GC35897 DPH A potent cell permeable c-Abl activator DPH  Chemical Structure
  91. GC35812 Dasatinib hydrochloride A potent and dual AblWT/Src inhibitor Dasatinib hydrochloride  Chemical Structure
  92. GC35753 CT-721 CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities. CT-721  Chemical Structure
  93. GC35682 CHMFL-ABL/KIT-155 CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis. CHMFL-ABL/KIT-155  Chemical Structure
  94. GC35651 Cenisertib Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia. Cenisertib  Chemical Structure
  95. GC35530 BJE6-106 BJE6-106 (B106) is a potent, selective 3rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM). BJE6-106  Chemical Structure
  96. GC35462 Bafetinib

    Bcr-Abl/Lyn tyrosine kinase inhibitor

    Bafetinib  Chemical Structure
  97. GC35442 Azaindole 1 Azaindole 1 (Azaindole 1; TC-S 7001) is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1nM for human ROCK-1 and ROCK-2, respectively. Azaindole 1  Chemical Structure
  98. GC35210 A 83-01 sodium salt A potent inhibitor of TGF-β type I receptor ALK5 kinase A 83-01 sodium salt  Chemical Structure
  99. GC44903 SMAD3 Inhibitor, SIS3 SMAD3 Inhibitor, SIS3 is a potent and selective inhibitor of Smad3 phosphorylation. SMAD3 Inhibitor, SIS3  Chemical Structure
  100. GC44729 Prostratin An HIV reactivator Prostratin  Chemical Structure
  101. GC44655 PKCε Inhibitor Peptide PKCε Inhibitor Peptide (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. PKCε Inhibitor Peptide  Chemical Structure

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