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. GC44729 Prostratin An HIV reactivator Prostratin  Chemical Structure
  3. 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
  4. 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
  5. 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
  6. GC11803 Pseudo RACK1 Activator of protein kinase C Pseudo RACK1  Chemical Structure
  7. 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
  8. GC14583 R 59-022 Diacylglycerol (DAG) kinase inhibitor R 59-022  Chemical Structure
  9. GC69792 R 59-022 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
  10. 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
  11. GC18246 R-59-949

    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
  12. GC11140 Radotinib(IY-5511) Bcr-Abl tyrosine kinase inhibitor Radotinib(IY-5511)  Chemical Structure
  13. GC16793 RepSox A selective inhibitor of ALK5 RepSox  Chemical Structure
  14. 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
  15. 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
  16. 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
  17. GC17322 Ro 31-8220 pan-PKC inhibitor Ro 31-8220  Chemical Structure
  18. GC17014 Ro 31-8220 Mesylate Pan-PKC inhibitor Ro 31-8220 Mesylate  Chemical Structure
  19. GC10029 Ro 31-8220 methanesulfonate 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
  20. GC13677 Ro 32-0432 hydrochloride protein kinase C inhibitor Ro 32-0432 hydrochloride  Chemical Structure
  21. 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
  22. 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
  23. 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
  24. 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
  25. GC10820 Rottlerin PKC inhibitor Rottlerin  Chemical Structure
  26. GC63177 Ruboxistaurin Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin  Chemical Structure
  27. GC16405 Safingol PKC and sphingosine kinases inhibitor Safingol  Chemical Structure
  28. 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
  29. GC13759 SAR407899 ATP-competitive ROCK inhibitor SAR407899  Chemical Structure
  30. GC16289 SAR407899 hydrochloride ATP-competitive ROCK inhibitor SAR407899 hydrochloride  Chemical Structure
  31. GC15197 Saracatinib (AZD0530) 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
  32. GC11022 SB 218078 checkpoint kinase 1 (Chk1) inhibitor SB 218078  Chemical Structure
  33. GC11545 SB 431542

    SB-431542, a small molecule inhibitor

    SB 431542  Chemical Structure
  34. GC15170 SB 772077B dihydrochloride Rho-kinase (ROCK) inhibitor SB 772077B dihydrochloride  Chemical Structure
  35. GC10421 SB-505124 hydrochloride Inhibitor of receptors ALK4, ALK5, and ALK7 SB-505124 hydrochloride  Chemical Structure
  36. GC13769 SB505124 ALK4/ALK5/ALK7 inhibitor SB505124  Chemical Structure
  37. GC14349 SB525334 (TGF-beta1) receptor inhibitor SB525334  Chemical Structure
  38. GC13320 SC-10 Protein kinase C activator SC-10  Chemical Structure
  39. GC18055 SC-9 protein kinase C activator SC-9  Chemical Structure
  40. GC13904 SD-208 A potent, selective inhibitor of TGF-βRI SD-208  Chemical Structure
  41. GC17191 SIS3 HCl SIS3HCl is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. SIS3 HCl  Chemical Structure
  42. 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
  43. GC32788 SJ000291942 A BMP signaling activator SJ000291942  Chemical Structure
  44. GC19447 SM 16

    SM 16 is a ALK5/ALK4 kinase inhibitor

    SM 16  Chemical Structure
  45. GC44903 SMAD3 Inhibitor, SIS3 SMAD3 Inhibitor, SIS3 is a potent and selective inhibitor of Smad3 phosphorylation. SMAD3 Inhibitor, SIS3  Chemical Structure
  46. 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
  47. GC15520 Sotrastaurin (AEB071) 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
  48. GC10722 SR-3677 Rho Kinase (ROCK-II) inhibitor SR-3677  Chemical Structure
  49. GC19338 SRI-011381 hydrochloride An oral bioavailabile TGF-beta signaling agonist SRI-011381 hydrochloride  Chemical Structure
  50. GC15299 Staurosporine(CGP 41251)

    A potent inhibitor of protein kinase C

    Staurosporine(CGP 41251)  Chemical Structure
  51. 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
  52. GC16821 TAE226(NVP-TAE226) 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
  53. GC17901 Tamoxifen Tamoxifen(TAM) serves as a selective estrogen receptor regulator (SERM), inhibiting estrogen's effects in breast cells while potentially stimulating estrogen activity in cells found in different tissues. Tamoxifen  Chemical Structure
  54. GC10682 TAS 301

    inhibitor of smooth muscle cell migration and proliferation, inhibits PKC signaling

    TAS 301  Chemical Structure
  55. GC11181 Thiazovivin ROCK inhibitor Thiazovivin  Chemical Structure
  56. 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
  57. GC70050 Trabedersen

    Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen can be used to study malignant brain tumors and other solid tumors that overexpress TGF-β2, such as skin, pancreatic, and colon tumors.

    Trabedersen  Chemical Structure
  58. GC40928 Trimethylamine N-oxide Trimethylamine N-oxide (TMAO) is a product of the oxidation of TMA by flavin-containing mono-oxygenase 3 in the liver. Trimethylamine N-oxide  Chemical Structure
  59. GC16678 UCN-02 protein kinase C inhibitor UCN-02  Chemical Structure
  60. 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
  61. GC16934 Valrubicin chemotherapy drug used to treat bladder cancer Valrubicin  Chemical Structure
  62. GC70110 Vamotinib

    Vamotinib (PF-114) is an effective, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the self-phosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib exhibits anti-proliferative and anti-tumor activity. Vamotinib has potential in the study of resistant Philadelphia chromosome-positive (Ph+) leukemia.

    Vamotinib  Chemical Structure
  63. GC13232 Verbascoside PKC/NF-κB inhibitor Verbascoside  Chemical Structure
  64. GC31912 VTX-27 VTX-27 is a selective protein kinase C θ (PKC θ) inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ. VTX-27  Chemical Structure
  65. GC26055 WAY-301398 WAY-301398 (6-methoxynaphthalene) can bind to protein kinase C (PKC). WAY-301398  Chemical Structure
  66. GC26065 WAY-354831 WAY-354831 exhibits antibacterial activity. WAY-354831  Chemical Structure
  67. GC10970 WP1130 WP1130 (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. WP1130 has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2. WP1130  Chemical Structure
  68. 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
  69. GC15712 Y-27632

    A ROCK inhibitor,potent and selective

    Y-27632  Chemical Structure
  70. 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
  71. GC13423 Y-39983 dihydrochloride ROCK family inhibitor Y-39983 dihydrochloride  Chemical Structure
  72. GC70166 Z-Arg-SBzl

    Z-Arg-SBzl is a substrate for activating protein C in both cows and humans.

    Z-Arg-SBzl  Chemical Structure
  73. GC33120 ZINC00881524 A ROCK inhibitor ZINC00881524  Chemical Structure
  74. GC13273 ZIP ZIP is a selective peptide inhibitor of PKMζ. ZIP  Chemical Structure
  75. GC13461 ZIP (SCRAMBLED) PKMζ inhibitor ZIP (SCRAMBLED)  Chemical Structure
  76. GC16510 ZIP, Biotinylated ZIP with a biotin moiety covalently attached ZIP, Biotinylated  Chemical Structure
  77. GC14701 Zoledronic Acid Potent nitrogen-containing bisphosphonates Zoledronic Acid  Chemical Structure
  78. GC17727 [Ala107]-MBP (104-118) Non-competitive inhibitor of PKC [Ala107]-MBP (104-118)  Chemical Structure
  79. GC15345 [Ala113]-MBP (104-118) Non-competitive inhibitor of PKC [Ala113]-MBP (104-118)  Chemical Structure
  80. GC10343 α-Amyloid Precursor Protein Modulator α-Amyloid Precursor Protein Modulator is a cell-permeable benzolactam-derived protein kinase C (PKC) activator with a Ki of 11.9 nM. α-Amyloid Precursor Protein Modulator  Chemical Structure
  81. 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

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