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. GC15079 GNF 5 Bcr-Abl inhibitor GNF 5  Chemical Structure
  3. GC10607 GNF-7

    Type II Bcr-Abl inhibitor

    GNF-7  Chemical Structure
  4. GC15564 Go 6976 PKCα/PKCβ1 inhibitor Go 6976  Chemical Structure
  5. GC16907 Go 6983

    Go 6983 (GÖ 6983) is one of the bisindolylmaleimide group of PKC inhibitor compounds, Go 6983 (GÖ 6983) was able to differentiate between PKC mu and other PKC isoenzymes.

    Go 6983  Chemical Structure
  6. GC38791 GSK-25 GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25  Chemical Structure
  7. GC19177 GSK180736A GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 uM. GSK180736A  Chemical Structure
  8. GC17936 GSK269962A ROCK inhibitor GSK269962A  Chemical Structure
  9. 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
  10. GC18119 GSK429286A Selective ROCK1/ROCK2 inhibitor GSK429286A  Chemical Structure
  11. GC11878 GW788388 ALK5 inhibitor,potent and selective GW788388  Chemical Structure
  12. GC10915 GZD824 Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 has antitumor activity. GZD824  Chemical Structure
  13. GC33201 GZD856 GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-AblT315I inhibitor, with IC50s of 19.9 and 15.4?nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity. GZD856  Chemical Structure
  14. 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
  15. 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
  16. GC31650 Halofuginone (RU-19110) Halofuginone (RU-19110) (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone (RU-19110)  Chemical Structure
  17. GC31950 Halofuginone hydrobromide (RU-19110 (hydrobromide)) Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromide (RU-19110 (hydrobromide))  Chemical Structure
  18. GC10299 Hexadecyl Methyl Glycerol protein kinase C activity inhibitor Hexadecyl Methyl Glycerol  Chemical Structure
  19. GC15018 Hispidin protein kinase Cβ inhibitor Hispidin  Chemical Structure
  20. GC64326 Hydrochlorothiazid-d2 Hydrochlorothiazid-d2  Chemical Structure
  21. GC17523 Hydrochlorothiazide diuretic drug of the thiazide class Hydrochlorothiazide  Chemical Structure
  22. 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
  23. GC15420 ICP 103 Protein kinase inhibitor ICP 103  Chemical Structure
  24. GC10314 Imatinib (STI571) Imatinib (STI571) (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib (STI571) also is an inhibitor of SARS-CoV and MERS-CoV. Imatinib (STI571)  Chemical Structure
  25. GC11759 Imatinib Mesylate (STI571) Imatinib Mesylate (STI571) (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases. Imatinib Mesylate (STI571)  Chemical Structure
  26. GC50317 IN 1130 Potent and selective inhibitor of TGF-βRI IN 1130  Chemical Structure
  27. GC32870 Ingenol ((-)-Ingenol) Ingenol ((-)-Ingenol) is a PKC activator, with a Ki of 30 μM, with antitumor activity. Ingenol ((-)-Ingenol)  Chemical Structure
  28. 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
  29. GC31656 Ingenol Mebutate (Ingenol 3-angelate) Ingenol Mebutate (Ingenol 3-angelate) is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity. Ingenol Mebutate (Ingenol 3-angelate)  Chemical Structure
  30. GC15148 Ionomycin calcium salt

    Lonomycin is a selective calcium ionophore derived from S. conglobatus that mobilizes intracellular calcium stores.

    Ionomycin calcium salt  Chemical Structure
  31. GC15446 Ionomycin free acid Ionomycin free acid (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin free acid  Chemical Structure
  32. GC60210 Isosaponarin Isosaponarin is a flavone glycoside isolated from wasabi leaves. Isosaponarin  Chemical Structure
  33. GC12108 ITD 1 First selective TGFβ inhibitor ITD 1  Chemical Structure
  34. GC11362 K 252a A protein kinase inhibitor K 252a  Chemical Structure
  35. GC15281 K-252c Protein kinase inhibitor K-252c  Chemical Structure
  36. GC15567 K02288 ALK inhibitor K02288  Chemical Structure
  37. GC43993 K252b K252b is an indolocarbazole isolated from the actinomycete Nocardiopsis, first described as an inhibitor of protein kinase C. K252b  Chemical Structure
  38. GC15057 Kartogenin Promote differentiation of multipotent MSCs into chondrocytes Kartogenin  Chemical Structure
  39. 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
  40. GC17346 KT 5823 A protein kinase G inhibitor KT 5823  Chemical Structure
  41. GC12817 K–115 hydrochloride dihydrate K-115 hydrochloride dihydrate (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively. K–115 hydrochloride dihydrate  Chemical Structure
  42. GC40770 L-erythro Sphingosine (d18:1) L-erythro Sphingosine is a synthetic stereoisomer of sphingosine (d18:1). L-erythro Sphingosine (d18:1)  Chemical Structure
  43. GC17815 L-threo-Sphingosine C-18 L-threo-Sphingosine C-18 is a potent MAPK inhibitor. L-threo-Sphingosine C-18 induces apoptosis and clear DNA fragmentation. L-threo-Sphingosine C-18 shows anticancer effect. L-threo-Sphingosine C-18  Chemical Structure
  44. GC16580 LDN-193189 ALK inhibitor,potent and selective LDN-193189  Chemical Structure
  45. GC17035 LDN-212854 BMP receptor inhibitor,potent and selective LDN-212854  Chemical Structure
  46. GC13225 LDN-214117 potent and selective ALK2 inhibitor LDN-214117  Chemical Structure
  47. GC14931 LDN193189 Hydrochloride An inhibitor of BMP receptors ALK1, ALK2, ALK3, and ALK6 LDN193189 Hydrochloride  Chemical Structure
  48. GC36433 LDN193189 Tetrahydrochloride A selective BMP type I receptor inhibitor LDN193189 Tetrahydrochloride  Chemical Structure
  49. 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
  50. GC32728 LSKL, Inhibitor of Thrombospondin TSP-1 LSKL, Inhibitor of Thrombospondin TSP-1 is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin TSP-1 inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin TSP-1 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 can readily crosse the blood-brain barrier. LSKL, Inhibitor of Thrombospondin TSP-1  Chemical Structure
  51. GC69412 Luspatercept

    Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that can bind to the ligands of the transforming growth factor β superfamily. Luspatercept increases red blood cell count and promotes maturation of red blood cell precursors. Luspatercept binds with GDF11, inhibiting the Smad2/3 signaling pathway. Luspatercept can be used for research on anemia.

    Luspatercept  Chemical Structure
  52. GC12402 LX7101 HCL LX7101 HCL is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM. LX7101 HCL  Chemical Structure
  53. GC32811 LXS196 LXS196 (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. LXS196 has the potential for uveal melanoma research. LXS196  Chemical Structure
  54. GC17563 LY 333531 hydrochloride Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). LY 333531 hydrochloride  Chemical Structure
  55. GC12363 LY2109761 TβRI/II kinase inhibitor LY2109761  Chemical Structure
  56. GC18015 LY2157299 LY2157299 (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM. LY2157299  Chemical Structure
  57. GC19234 LY3200882 LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). LY3200882  Chemical Structure
  58. GC11604 LY364947

    Inhibitor of TGF-β type I receptor kinase domain

    LY364947  Chemical Structure
  59. GC30545 Malantide Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM. Malantide  Chemical Structure
  60. GC10496 Midostaurin (PKC412) Midostaurin (PKC412) (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin (PKC412) inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM. Midostaurin (PKC412) also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin (PKC412) shows powerful anticancer effects. Midostaurin (PKC412)  Chemical Structure
  61. GC32714 Mitoxantrone (mitozantrone) Mitoxantrone (mitozantrone) is a potent topoisomerase II inhibitor. Mitoxantrone (mitozantrone)  Chemical Structure
  62. GC14363 Mitoxantrone HCl Mitoxantrone HCl is a potent topoisomerase II inhibitor. Mitoxantrone HCl  Chemical Structure
  63. GC17582 ML347 BMP receptor inhibitor,potent and selective ML347  Chemical Structure
  64. GC65585 Mongersen Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen  Chemical Structure
  65. 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
  66. GC49269 Myr-ZIP A PKMζ inhibitor Myr-ZIP  Chemical Structure
  67. GC44303 N-Acetylpuromycin N-Acetylpuromycin is a non-ribotoxic form of the antibiotic puromycin that is formed in puromycin-resistant S. N-Acetylpuromycin  Chemical Structure
  68. 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
  69. 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
  70. GC10716 Netarsudil (AR-13324) ROCK inhibitor Netarsudil (AR-13324)  Chemical Structure
  71. GC13514 NG25 An inhibitor of MAP4K2 and TAK1 NG25  Chemical Structure
  72. 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
  73. GC14075 Nocodazole A tubulin production inhibitor,anti-neoplastic agent Nocodazole  Chemical Structure
  74. 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
  75. 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
  76. GN10378 Oxymatrine Oxymatrine  Chemical Structure
  77. 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
  78. GC12637 PD 180970 P210bcr/abl tyrosine kinase inhibitor PD 180970  Chemical Structure
  79. GC13592 PD173955 Dual Src/Abl kinase inhibitor, ATP-competitive, PD173955  Chemical Structure
  80. GC33901 Pentanoic acid Pentanoic acid  Chemical Structure
  81. GC61585 Pep2m, myristoylated TFA Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide. Pep2m, myristoylated TFA  Chemical Structure
  82. GC14767 PF-00562271 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
  83. GC14407 PF-431396 Pyk2 and FAK inhibitor PF-431396  Chemical Structure
  84. GC15380 PF-562271 ATP-competitive FAK inhibitor, reversible PF-562271  Chemical Structure
  85. GC10810 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
  86. GC17352 Phorbol 12,13-dibutyrate Protein kinase C activator Phorbol 12,13-dibutyrate  Chemical Structure
  87. GC12790 Pirfenidone TGF-β production inhibitor Pirfenidone  Chemical Structure
  88. 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
  89. GC15471 PKC β pseudosubstrate Selective cell-permeable peptide inhibitor of protein kinase C PKC β pseudosubstrate  Chemical Structure
  90. GC10404 PKC ζ pseudosubstrate PKC ζ pseudosubstrate is a selective cell-permeable inhibitor of PKC. PKC ζ pseudosubstrate  Chemical Structure
  91. GC11671 PKC fragment (530-558) Potent activator of protein kinase C PKC fragment (530-558)  Chemical Structure
  92. GC44655 PKCε Inhibitor Peptide PKCε Inhibitor Peptide (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. PKCε Inhibitor Peptide  Chemical Structure
  93. 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
  94. 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
  95. GC30200 PKC-theta inhibitor PKC-theta inhibitor is a selective PKC-θinhibitor, with an IC50 of 12 nM. PKC-theta inhibitor  Chemical Structure
  96. GC67686 PKCiota-IN-2 formic PKCiota-IN-2 formic  Chemical Structure
  97. GC14396 Ponatinib (AP24534) 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
  98. GC45828 Ponatinib-d8 An internal standard for the quantification of ponatinib Ponatinib-d8  Chemical Structure
  99. GC68339 Ponsegromab Ponsegromab  Chemical Structure
  100. GC12779 PPY A Abl kinases inhibitor PPY A  Chemical Structure
  101. 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

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