TGF-beta/Smad

Choose Selective TGF-beta/Smad Inhibitors

TGF-beta/Smad Signaling Pathway Map

TGF-beta/Smad Signaling Pathways

TGF-beta/Smad Products

  • All (40)
  • TGF-beta/Smad Inhibitors (31)
  • TGF-beta/Smad Antibodie (1)
  • TGF-beta/Smad Activators (4)
  • TGF-beta/Smad Agonists (2)
  • TGF-beta/Smad Modulators (2)
  • New TGF-beta/Smad Products
Catalog No. Product Name Information Product Use Citations Product Validations
S0752 AUDA AUDA (compound 43) is a potent inhibitor of soluble epoxide hydrolase (sEH) with IC50 of 18 nM and 69 nM for the mouse sEH and human sEH, respectively. AUDA has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. AUDA downregulates Smad3 and p38 signaling pathways.
S1067 SB431542 SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM in a cell-free assay, 100-fold more selective for ALK5 than p38 MAPK and other kinases.
Adv Mater, 2022, e2106829
Adv Sci (Weinh), 2022, e2103939
Adv Sci (Weinh), 2022, e2106075
S1476 SB525334 SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM in a cell-free assay, 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.
FASEB J, 2022, 36(2):e22124
Sci Rep, 2022, 12(1):7
Cancer Commun (Lond), 2022, 42(1):17-36
S1576 Sulfasalazine (NSC 667219) Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.
Cell Mol Life Sci, 2022, 79(5):228
Front Bioeng Biotechnol, 2022, 10:855755
Cell Metab, 2021, S1550-4131(21)00233-3
S2186 SB505124 SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM in cell-free assays, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6.
Blood Cancer J, 2022, 12(3):39
Sci Rep, 2022, 12(1):7
Biomaterials, 2021, 274:120856
S2230 Galunisertib (LY2157299) Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3.
Cancer Cell, 2022, S1535-6108(21)00662-0
Int J Biol Sci, 2022, 18(5):1912-1932
Arch Toxicol, 2022, 10.1007/s00204-022-03265-7
S2234 BIBF-0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34nM.
S2618 LDN-193189 LDN-193189 (DM3189) is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. For animal testing, the water-soluble S7507 LDN-193189 2HCl is recommended.
Adv Mater, 2022, e2106829
Adv Sci (Weinh), 2022, e2106075
Stem Cell Res Ther, 2022, 13(1):120
S2704 LY2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. LY2109761 blocks autophagy and induces apoptosis.
Nat Immunol, 2022, 23(2):237-250
Nat Commun, 2022, 13(1):1017
Cell Mol Life Sci, 2022, 79(3):153
S2750 GW788388 GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM in a cell-free assay, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.
Sci Rep, 2022, 12(1):7
EMBO Mol Med, 2021, 13(6):e13270
iScience, 2021, 24(10):103193
S2805 LY364947 LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.
Cell Rep, 2022, 38(5):110329
Aging Dis, 2022, 13(1):313-328
Dis Model Mech, 2022, dmm.046979
S2907 Pirfenidone (S-7701) Pirfenidone (S-7701, AMR-69) is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.
Cancer Biol Ther, 2022, 23(1):150-162
Sci Rep, 2022, 12(1):7
Integr Biol (Camb), 2022, 14(1):1-12
S5183 PD 169316 PD 169316 is a potent, selective and cell-permeable p38 MAP kinase inhibitor with IC50 of 89 nM. PD169316 abrogates signaling initiated by both TGFbeta and Activin A. PD169316 shows antiviral activity against Enterovirus71.
PLoS One, 2021, 16(5):e0252541
S6713 ITD-1 ITD-1 is a potent TGF-β inhibitor. It does not block the kinase activity of either type I (TGFBR1) or type II (TGFBR2) TGFβ receptors but potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2, and only minimally in response to Activin A.
Nat Commun, 2022, 13(1):438
J Exp Clin Cancer Res, 2021, 40(1):62
J Mol Cell Cardiol, 2020, 3;142:53-64
S6807 TA-02 TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2.
S7146 DMH1 DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. DMH1 inhibits autophagy.
Nat Commun, 2021, 12(1):6374
Proc Natl Acad Sci U S A, 2021, 118(29)e2101783118
Cell Rep, 2021, 34(12):108889
S7147 LDN-212854 LDN-212854 (BMP Inhibitor III) is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively.
Nat Commun, 2021, 12(1):6177
Mol Oncol, 2021, 10.1002/1878-0261.12963
Mol Med Rep, 2020, 21(1):61-68
S7148 ML347 ML347 (LDN-193719) is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM.
Biomolecules, 2020, 10(4)E519
Biomolecules, 2020, 29;10(4) pii: E519
eNeuro, 2020, 7(5):ENEURO.0104-20.2020
S7223 RepSox (E-616452) RepSox (E-616452, SJN 2511, ALK5 Inhibitor II) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively.
Sci Adv, 2022, 8(8):eabj6621
Biomater Sci, 2022, 10.1039/d1bm01287h
Sci Rep, 2022, 12(1):7
S7306 Dorsomorphin (Compound C) 2HCl Dorsomorphin 2HCl (BML-275, Compound C) is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line.
Signal Transduct Target Ther, 2022, 7(1):66
Redox Biol, 2022, 52:102288
Brain Behav Immun, 2022, S0889-1591(22)00041-1
S7359 K02288 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, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.
Sci Rep, 2022, 12(1):7
Nat Commun, 2021, 12(1):6177
Mol Oncol, 2021, 10.1002/1878-0261.12963
S7507 LDN-193189 2HCl LDN-193189 (DM3189) 2HCl is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.
Adv Mater, 2022, e2106829
Adv Sci (Weinh), 2022, e2106075
Redox Biol, 2022, 50:102248
S7530 Vactosertib (TEW-7197) Vactosertib  (TEW-7197, EW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.
Cancer Cell, 2021, S1535-6108(21)00492-X
Cell Rep, 2021, 34(12):108882
Biomater Sci, 2021, 10.1039/d1bm01699g
S7624 SD-208 SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
Acta Biomater, 2022, S1742-7061(22)00004-6
Cardiovasc Res, 2021, cvab205
J Clin Invest, 2020, 130(3):1377-1391
S7627 LDN-214117 LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.
FASEB J, 2021, 35(3):e21263
Stem Cells Int, 2019, 2019:5026793
S7692 A-83-01 A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions are best fresh-prepared.
Sci Adv, 2021, 7(51):eabh0562
Sci Adv, 2021, 7(33)eabf4416
Biomaterials, 2021, 280:121266
S7840 Dorsomorphin (Compound C) Dorsomorphin (Compound C, BML-275) is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For animal testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.
Signal Transduct Target Ther, 2022, 7(1):66
Brain Behav Immun, 2022, S0889-1591(22)00041-1
Free Radic Biol Med, 2022, 182:219-231
S7959 SIS3 HCl SIS3, a novel specific inhibitor of Smad3, inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways.
Nat Immunol, 2022, 23(2):237-250
J Biol Chem, 2022, 298(4):101748
Biol Trace Elem Res, 2022, 10.1007/s12011-022-03169-8
S8144 Halofuginone Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.
Gastric Cancer, 2021, 10.1007/s10120-021-01259-5
Research Square, 2021, 10.21203/rs.3.rs-738132/v1
Sci Rep, 2020, 10(1):19723
S8700 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.
Commun Biol, 2021, 4(1):318
Stem Cell Res Ther, 2020, 11(1):365
Mol Med Rep, 2019, 10.3892/mmr.2019.10655
S8772 LY 3200882 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.
J Inflamm Res, 2021, 14:2897-2911
Pediatr Rheumatol Online J, 2021, 19(1):72
Br J Cancer, 2020, 10.1038/s41416-020-01040-y
A5130 Smad4 Rabbit Recombinant mAb Smad4 Rabbit Recombinant mAb detects endogenous level of total Smad4.
S0153 SJ000291942 SJ000291942 is a canonical bone morphogenetic proteins (BMP) signaling pathway activator.
S3223 L-Quebrachitol L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation and cell DNA synthesis. L-Quebrachitol upregulates bone morphogenetic protein-2 (BMP-2) and runt-related transcription factor-2 (Runx2) and regulatory genes associated with mitogen-activated protein kinase (MAPK) and Wnt/β-catenin signaling pathway, while down-regulating the receptor activator of the nuclear factor-κB(NF-κB) ligand (RANKL) mRNA level.
S7658 Kartogenin Kartogenin (KGN) is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.
Acta Biomater, 2021, S1742-7061(21)00015-5
Anticancer Res, 2021, 41(10):4753-4759
Front Chem, 2019, 7:677
S7914 Isoxazole 9 (ISX-9) Isoxazole 9 (Isx-9) is a synthetic promotor of adult neurogenesis by triggering neuronal differentiation of adult neural stem/precursor cells (NSPCs). Isoxazole 9 (Isx-9) activates multiple pathways including TGF-β induced epithelial–mesenchymal transition (EMT) signaling, canonical and non-canonical Wnt signaling at different stages of cardiac differentiation.
Front Cell Dev Biol, 2021, 9:728352
S0523 SB 4 SB 4 is a potent and selective agonist of bone morphogenetic protein 4 (BMP4) signaling with EC50 of 74 nM. SB 4 enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation.
S6654 SRI-011381 SRI-011381 is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease.
Dis Model Mech, 2022, dmm.046979
Front Cell Dev Biol, 2021, 9:648201
Eur J Pharmacol, 2021, 912:174587
S2308 Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.
Sci Rep, 2022, 12(1):7
Front Pharmacol, 2021, 12:735087
Carcinogenesis, 2020, 41(7):993-1004
S8318 Alantolactone Alantolactone (helenin, helenine, Eupatal), a naturally occurring eudesmane-type sesquiterpene lactone (SL), could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction.
Nat Commun, 2022, 13(1):107
Onco Targets Ther, 2017, 10:1767-1776
S0752 AUDA AUDA (compound 43) is a potent inhibitor of soluble epoxide hydrolase (sEH) with IC50 of 18 nM and 69 nM for the mouse sEH and human sEH, respectively. AUDA has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. AUDA downregulates Smad3 and p38 signaling pathways.
S1067 SB431542 SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM in a cell-free assay, 100-fold more selective for ALK5 than p38 MAPK and other kinases.
Adv Mater, 2022, e2106829
Adv Sci (Weinh), 2022, e2103939
Adv Sci (Weinh), 2022, e2106075
S1476 SB525334 SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM in a cell-free assay, 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.
FASEB J, 2022, 36(2):e22124
Sci Rep, 2022, 12(1):7
Cancer Commun (Lond), 2022, 42(1):17-36
S1576 Sulfasalazine (NSC 667219) Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.
Cell Mol Life Sci, 2022, 79(5):228
Front Bioeng Biotechnol, 2022, 10:855755
Cell Metab, 2021, S1550-4131(21)00233-3
S2186 SB505124 SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM in cell-free assays, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6.
Blood Cancer J, 2022, 12(3):39
Sci Rep, 2022, 12(1):7
Biomaterials, 2021, 274:120856
S2230 Galunisertib (LY2157299) Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3.
Cancer Cell, 2022, S1535-6108(21)00662-0
Int J Biol Sci, 2022, 18(5):1912-1932
Arch Toxicol, 2022, 10.1007/s00204-022-03265-7
S2234 BIBF-0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34nM.
S2618 LDN-193189 LDN-193189 (DM3189) is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. For animal testing, the water-soluble S7507 LDN-193189 2HCl is recommended.
Adv Mater, 2022, e2106829
Adv Sci (Weinh), 2022, e2106075
Stem Cell Res Ther, 2022, 13(1):120
S2704 LY2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. LY2109761 blocks autophagy and induces apoptosis.
Nat Immunol, 2022, 23(2):237-250
Nat Commun, 2022, 13(1):1017
Cell Mol Life Sci, 2022, 79(3):153
S2750 GW788388 GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM in a cell-free assay, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.
Sci Rep, 2022, 12(1):7
EMBO Mol Med, 2021, 13(6):e13270
iScience, 2021, 24(10):103193
S2805 LY364947 LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II.
Cell Rep, 2022, 38(5):110329
Aging Dis, 2022, 13(1):313-328
Dis Model Mech, 2022, dmm.046979
S2907 Pirfenidone (S-7701) Pirfenidone (S-7701, AMR-69) is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.
Cancer Biol Ther, 2022, 23(1):150-162
Sci Rep, 2022, 12(1):7
Integr Biol (Camb), 2022, 14(1):1-12
S5183 PD 169316 PD 169316 is a potent, selective and cell-permeable p38 MAP kinase inhibitor with IC50 of 89 nM. PD169316 abrogates signaling initiated by both TGFbeta and Activin A. PD169316 shows antiviral activity against Enterovirus71.
PLoS One, 2021, 16(5):e0252541
S6713 ITD-1 ITD-1 is a potent TGF-β inhibitor. It does not block the kinase activity of either type I (TGFBR1) or type II (TGFBR2) TGFβ receptors but potently blocks phosphorylation of the effector SMAD2/3 proteins induced by TGFβ2, and only minimally in response to Activin A.
Nat Commun, 2022, 13(1):438
J Exp Clin Cancer Res, 2021, 40(1):62
J Mol Cell Cardiol, 2020, 3;142:53-64
S6807 TA-02 TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2.
S7146 DMH1 DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. DMH1 inhibits autophagy.
Nat Commun, 2021, 12(1):6374
Proc Natl Acad Sci U S A, 2021, 118(29)e2101783118
Cell Rep, 2021, 34(12):108889
S7147 LDN-212854 LDN-212854 (BMP Inhibitor III) is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively.
Nat Commun, 2021, 12(1):6177
Mol Oncol, 2021, 10.1002/1878-0261.12963
Mol Med Rep, 2020, 21(1):61-68
S7148 ML347 ML347 (LDN-193719) is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM.
Biomolecules, 2020, 10(4)E519
Biomolecules, 2020, 29;10(4) pii: E519
eNeuro, 2020, 7(5):ENEURO.0104-20.2020
S7223 RepSox (E-616452) RepSox (E-616452, SJN 2511, ALK5 Inhibitor II) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively.
Sci Adv, 2022, 8(8):eabj6621
Biomater Sci, 2022, 10.1039/d1bm01287h
Sci Rep, 2022, 12(1):7
S7306 Dorsomorphin (Compound C) 2HCl Dorsomorphin 2HCl (BML-275, Compound C) is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line.
Signal Transduct Target Ther, 2022, 7(1):66
Redox Biol, 2022, 52:102288
Brain Behav Immun, 2022, S0889-1591(22)00041-1
S7359 K02288 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, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.
Sci Rep, 2022, 12(1):7
Nat Commun, 2021, 12(1):6177
Mol Oncol, 2021, 10.1002/1878-0261.12963
S7507 LDN-193189 2HCl LDN-193189 (DM3189) 2HCl is a selective BMP signaling inhibitor, inhibits the ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8 nM, 0.8 nM, 5.3 nM and 16.7 nM in the kinase assay, respectively. LDN-193189 inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50s of 5 nM and 30 nM in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.
Adv Mater, 2022, e2106829
Adv Sci (Weinh), 2022, e2106075
Redox Biol, 2022, 50:102248
S7530 Vactosertib (TEW-7197) Vactosertib  (TEW-7197, EW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.
Cancer Cell, 2021, S1535-6108(21)00492-X
Cell Rep, 2021, 34(12):108882
Biomater Sci, 2021, 10.1039/d1bm01699g
S7624 SD-208 SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
Acta Biomater, 2022, S1742-7061(22)00004-6
Cardiovasc Res, 2021, cvab205
J Clin Invest, 2020, 130(3):1377-1391
S7627 LDN-214117 LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.
FASEB J, 2021, 35(3):e21263
Stem Cells Int, 2019, 2019:5026793
S7692 A-83-01 A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions are best fresh-prepared.
Sci Adv, 2021, 7(51):eabh0562
Sci Adv, 2021, 7(33)eabf4416
Biomaterials, 2021, 280:121266
S7840 Dorsomorphin (Compound C) Dorsomorphin (Compound C, BML-275) is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For animal testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.
Signal Transduct Target Ther, 2022, 7(1):66
Brain Behav Immun, 2022, S0889-1591(22)00041-1
Free Radic Biol Med, 2022, 182:219-231
S7959 SIS3 HCl SIS3, a novel specific inhibitor of Smad3, inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways.
Nat Immunol, 2022, 23(2):237-250
J Biol Chem, 2022, 298(4):101748
Biol Trace Elem Res, 2022, 10.1007/s12011-022-03169-8
S8144 Halofuginone Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.
Gastric Cancer, 2021, 10.1007/s10120-021-01259-5
Research Square, 2021, 10.21203/rs.3.rs-738132/v1
Sci Rep, 2020, 10(1):19723
S8700 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.
Commun Biol, 2021, 4(1):318
Stem Cell Res Ther, 2020, 11(1):365
Mol Med Rep, 2019, 10.3892/mmr.2019.10655
S8772 LY 3200882 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.
J Inflamm Res, 2021, 14:2897-2911
Pediatr Rheumatol Online J, 2021, 19(1):72
Br J Cancer, 2020, 10.1038/s41416-020-01040-y
A5130 Smad4 Rabbit Recombinant mAb Smad4 Rabbit Recombinant mAb detects endogenous level of total Smad4.
S0153 SJ000291942 SJ000291942 is a canonical bone morphogenetic proteins (BMP) signaling pathway activator.
S3223 L-Quebrachitol L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation and cell DNA synthesis. L-Quebrachitol upregulates bone morphogenetic protein-2 (BMP-2) and runt-related transcription factor-2 (Runx2) and regulatory genes associated with mitogen-activated protein kinase (MAPK) and Wnt/β-catenin signaling pathway, while down-regulating the receptor activator of the nuclear factor-κB(NF-κB) ligand (RANKL) mRNA level.
S7658 Kartogenin Kartogenin (KGN) is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.
Acta Biomater, 2021, S1742-7061(21)00015-5
Anticancer Res, 2021, 41(10):4753-4759
Front Chem, 2019, 7:677
S7914 Isoxazole 9 (ISX-9) Isoxazole 9 (Isx-9) is a synthetic promotor of adult neurogenesis by triggering neuronal differentiation of adult neural stem/precursor cells (NSPCs). Isoxazole 9 (Isx-9) activates multiple pathways including TGF-β induced epithelial–mesenchymal transition (EMT) signaling, canonical and non-canonical Wnt signaling at different stages of cardiac differentiation.
Front Cell Dev Biol, 2021, 9:728352
S0523 SB 4 SB 4 is a potent and selective agonist of bone morphogenetic protein 4 (BMP4) signaling with EC50 of 74 nM. SB 4 enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation.
S6654 SRI-011381 SRI-011381 is a novel agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease.
Dis Model Mech, 2022, dmm.046979
Front Cell Dev Biol, 2021, 9:648201
Eur J Pharmacol, 2021, 912:174587
S2308 Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.
Sci Rep, 2022, 12(1):7
Front Pharmacol, 2021, 12:735087
Carcinogenesis, 2020, 41(7):993-1004
S8318 Alantolactone Alantolactone (helenin, helenine, Eupatal), a naturally occurring eudesmane-type sesquiterpene lactone (SL), could induce activin/SMAD3 signaling and disrupt Cripto-1/activin receptor type II A interaction.
Nat Commun, 2022, 13(1):107
Onco Targets Ther, 2017, 10:1767-1776
Tags: TGF-beta inhibition | Smad inhibition | TGF-beta signaling | TGF-beta pathway | TGF-beta cancer | Smad signaling | Smad pathway | TGF-beta tumor | TGF-beta activation | TGF-beta family | Smad2 signaling | TGF-beta Smad signaling | Smad3 signaling | Smad cancer | Smad phosphorylation | Smad activation | Smad2 phosphorylation | Smad family | TGF-beta assay | Smad3 phosphorylation | TGF-beta inhibitor clinical trial | TGF-beta inhibitor review