TGF-beta/Smad

TGF-beta/Smad Products

  • All (45)
  • TGF-beta/Smad Inhibitors (37)
  • 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
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.
Nature, 2024, 10.1038/s41586-024-07067-y
Nat Methods, 2024, 10.1038/s41592-024-02172-2
Nat Commun, 2024, 15(1):1351
S7306 Dorsomorphin 2HCl Dorsomorphin 2HCl 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.
Adv Sci (Weinh), 2024, 11(4):e2304987
Genome Biol, 2024, 25(1):58
Cell Death Discov, 2024, 10(1):95
S7840 Dorsomorphin Dorsomorphin 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.
iScience, 2024, 27(2):108852
J Ethnopharmacol, 2024, 324:117814
J Cell Mol Med, 2024, 28(2):e18055
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.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
Regen Ther, 2024, 25:229-237
Stem Cell Res, 2024, 74:103271
Stem Cell Res, 2024, 74:103296
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.
Nat Commun, 2023, 14(1):3593
Cell Rep, 2023, 42(7):112804
Oncogene, 2023, 42(22):1857-1873
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.
Int J Mol Sci, 2024, 25(2)959
Mol Cancer, 2023, 22(1):66
Cells, 2023, 12(12)1624
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.
Cancer Res, 2023, 83(18):3095-3114
Cell Rep, 2023, 42(3):112162
Br J Cancer, 2023, none
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.
Cell Res, 2023, 10.1038/s41422-023-00846-8
Stem Cell Res Ther, 2023, 14(1):378
Front Cell Dev Biol, 2023, 11:1236243
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.
Int J Biol Sci, 2024, 20(1):200-217
Nat Commun, 2023, 14(1):1794
Nature Communications-, 2023, 1794-2023)
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.
Neuron, 2023, 111(9):1381-1390.e6
Cancer Sci, 2023, 10.1111/cas.15987
Neural Regen Res, 2023, 18(5):1090-1098
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.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Rep Med, 2024, 5(2):101416
Cell Rep, 2023, 42(6):112566
S2907 Pirfenidone Pirfenidone 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.
Eur Respir J, 2024, 2300580
Acta Pharmacol Sin, 2023, 10.1038/s41401-023-01156-w
Front Immunol, 2023, 14:1070196
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.
Neural Regen Res, 2024, 19(1):205-211
iScience, 2024, 27(3):109166
Commun Biol, 2023, 6(1):824
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.
Nat Commun, 2023, 14(1):4417
Nat Commun, 2023, 14(1):143
Nat Commun, 2023, 14(1):4417
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.
J Biol Chem, 2023, 299(4):103017
Cell Rep, 2022, 40(13):111423
Sci Rep, 2022, 12(1):7
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 unstable and should be fresh-prepared.
Nat Commun, 2024, 15(1):668
Nat Commun, 2024, 15(1):583
Stem Cell Reports, 2024, 19(2):196-210
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.
FEBS J, 2024, 291(2):272-291
J Neurooncol, 2024, 10.1007/s11060-024-04625-2
Int J Mol Sci, 2022, 23(3)1475
S7624 SD-208 SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
JCI Insight, 2023, 8(3)e166688
Cancers (Basel), 2023, 10.3390/cancers15205086
Cancers (Basel), 2023, 15(20)5086
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.
bioRxiv, 2023, 10.1101/2023.12.14.571626
Res Sq, 2023, rs.3.rs-3112163
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
S1576 Sulfasalazine Sulfasalazine 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.
Adv Sci (Weinh), 2023, 10(20):e2300517
Proc Natl Acad Sci U S A, 2022, 119(36):e2117396119
Cell Mol Life Sci, 2022, 79(5):228
S3552 SIS3 SIS3 is a cell-permeable inhibitor of Smad3 that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling. SIS3 reduces TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.
Front Bioeng Biotechnol, 2023, 11:1281157
Front Bioeng Biotechnol, 2023, 11:1281157
J Dent Sci, 2023, 18(1):87-94
S7658 Kartogenin Kartogenin (KGN) is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.
Pharmaceutics, 2023, 15(7)1949
Int J Mol Sci, 2022, 24(1)390
Front Pharmacol, 2022, 13:922032
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.
Front Pharmacol, 2024, 15:1257941
Cell Mol Biol Lett, 2023, 28(1):32
J Cell Commun Signal, 2023, 10.1007/s12079-023-00766-7
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.
Infect Agent Cancer, 2023, 18(1):27
FASEB J, 2022, 36(11):e22580
Invest Ophthalmol Vis Sci, 2022, 63(8):1
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.
Am J Pathol, 2023, S0002-9440(23)00047-0
Am J Pathol, 2023, 193(5):532-547
Int J Mol Sci, 2022, 23(3)1475
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
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.
Development, 2022, 149(20)dev192310
Biomolecules, 2020, 10(4)E519
Biomolecules, 2020, 29;10(4) pii: E519
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, 2023, 6(1):824
Nutrients, 2023, 16(1)64
Int J Mol Sci, 2023, 24(19)14444
S6654 SRI-011381 (C381) SRI-011381 (C381) 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
S7627 LDN-214117 LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.
bioRxiv, 2023, 2023.06.14.544941
FASEB J, 2021, 35(3):e21263
Stem Cells Int, 2019, 2019:5026793
S2308 Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.
J Transl Med, 2024, 22(1):208
Sci Rep, 2022, 12(1):7
Front Pharmacol, 2021, 12:735087
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.
Commun Biol, 2022, 5(1):750
Front Cell Dev Biol, 2021, 9:728352
Front Cell Dev Biol, 2021, 9:728352
S8318 Alantolactone Alantolactone, 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
E2394 TGFβRI-IN-3 TGFβRI-IN-3 represents a highly selective TGFβR1 inhibitor that has potential applications in immuno-oncology, inhibits TGFβR1 at an IC50 of 0.79 nM with 2000-fold selectivity against MAP4K4.
JCI Insight, 2023, e161563
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
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.
E4432New 3,3-Dimethyl-1-butanol 3,3-Dimethyl-1-butanol (Neohexanol) is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO). 3,3-dimethyl-1-butanol negatively inhibits the signalling pathways of p65 NF-κB and  TGF-β1/Smad3. 3,3-dimethyl-1-butanol has potential applications in cardiovascular disease (CVD).
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.
E3859 Lycopus Extract Lycopus Extract is extracted from Lycopus, which ameliorate podocytes injury by inhibiting TGF-β signaling pathway.
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.
S2234 BIBF-0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34nM.
E0769 Ginsenoside Rh4 Ginsenoside Rh4 is an important active ingredient of traditional Chinese medicine ginseng, which has been shown to inhibit Wnt/β-Catenin, JAK2/STAT3, TGF-β/Smad2/3 and other signaling pathways.
S0153 SJ000291942 SJ000291942 is a canonical bone morphogenetic proteins (BMP) signaling pathway activator.
S7710 R-268712 R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
S6807 TA-02 TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2.
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.
Nature, 2024, 10.1038/s41586-024-07067-y
Nat Methods, 2024, 10.1038/s41592-024-02172-2
Nat Commun, 2024, 15(1):1351
S7306 Dorsomorphin 2HCl Dorsomorphin 2HCl 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.
Adv Sci (Weinh), 2024, 11(4):e2304987
Genome Biol, 2024, 25(1):58
Cell Death Discov, 2024, 10(1):95
S7840 Dorsomorphin Dorsomorphin 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.
iScience, 2024, 27(2):108852
J Ethnopharmacol, 2024, 324:117814
J Cell Mol Med, 2024, 28(2):e18055
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.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
Regen Ther, 2024, 25:229-237
Stem Cell Res, 2024, 74:103271
Stem Cell Res, 2024, 74:103296
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.
Nat Commun, 2023, 14(1):3593
Cell Rep, 2023, 42(7):112804
Oncogene, 2023, 42(22):1857-1873
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.
Int J Mol Sci, 2024, 25(2)959
Mol Cancer, 2023, 22(1):66
Cells, 2023, 12(12)1624
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.
Cancer Res, 2023, 83(18):3095-3114
Cell Rep, 2023, 42(3):112162
Br J Cancer, 2023, none
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.
Cell Res, 2023, 10.1038/s41422-023-00846-8
Stem Cell Res Ther, 2023, 14(1):378
Front Cell Dev Biol, 2023, 11:1236243
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.
Int J Biol Sci, 2024, 20(1):200-217
Nat Commun, 2023, 14(1):1794
Nature Communications-, 2023, 1794-2023)
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.
Neuron, 2023, 111(9):1381-1390.e6
Cancer Sci, 2023, 10.1111/cas.15987
Neural Regen Res, 2023, 18(5):1090-1098
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.
Adv Sci (Weinh), 2024, 11(4):e2304987
Cell Rep Med, 2024, 5(2):101416
Cell Rep, 2023, 42(6):112566
S2907 Pirfenidone Pirfenidone 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.
Eur Respir J, 2024, 2300580
Acta Pharmacol Sin, 2023, 10.1038/s41401-023-01156-w
Front Immunol, 2023, 14:1070196
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.
Neural Regen Res, 2024, 19(1):205-211
iScience, 2024, 27(3):109166
Commun Biol, 2023, 6(1):824
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.
Nat Commun, 2023, 14(1):4417
Nat Commun, 2023, 14(1):143
Nat Commun, 2023, 14(1):4417
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.
J Biol Chem, 2023, 299(4):103017
Cell Rep, 2022, 40(13):111423
Sci Rep, 2022, 12(1):7
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 unstable and should be fresh-prepared.
Nat Commun, 2024, 15(1):668
Nat Commun, 2024, 15(1):583
Stem Cell Reports, 2024, 19(2):196-210
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.
FEBS J, 2024, 291(2):272-291
J Neurooncol, 2024, 10.1007/s11060-024-04625-2
Int J Mol Sci, 2022, 23(3)1475
S7624 SD-208 SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
JCI Insight, 2023, 8(3)e166688
Cancers (Basel), 2023, 10.3390/cancers15205086
Cancers (Basel), 2023, 15(20)5086
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.
bioRxiv, 2023, 10.1101/2023.12.14.571626
Res Sq, 2023, rs.3.rs-3112163
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00932-4
S1576 Sulfasalazine Sulfasalazine 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.
Adv Sci (Weinh), 2023, 10(20):e2300517
Proc Natl Acad Sci U S A, 2022, 119(36):e2117396119
Cell Mol Life Sci, 2022, 79(5):228
S3552 SIS3 SIS3 is a cell-permeable inhibitor of Smad3 that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling. SIS3 reduces TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.
Front Bioeng Biotechnol, 2023, 11:1281157
Front Bioeng Biotechnol, 2023, 11:1281157
J Dent Sci, 2023, 18(1):87-94
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.
Front Pharmacol, 2024, 15:1257941
Cell Mol Biol Lett, 2023, 28(1):32
J Cell Commun Signal, 2023, 10.1007/s12079-023-00766-7
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.
Infect Agent Cancer, 2023, 18(1):27
FASEB J, 2022, 36(11):e22580
Invest Ophthalmol Vis Sci, 2022, 63(8):1
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.
Am J Pathol, 2023, S0002-9440(23)00047-0
Am J Pathol, 2023, 193(5):532-547
Int J Mol Sci, 2022, 23(3)1475
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
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.
Development, 2022, 149(20)dev192310
Biomolecules, 2020, 10(4)E519
Biomolecules, 2020, 29;10(4) pii: E519
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, 2023, 6(1):824
Nutrients, 2023, 16(1)64
Int J Mol Sci, 2023, 24(19)14444
S7627 LDN-214117 LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.
bioRxiv, 2023, 2023.06.14.544941
FASEB J, 2021, 35(3):e21263
Stem Cells Int, 2019, 2019:5026793
E2394 TGFβRI-IN-3 TGFβRI-IN-3 represents a highly selective TGFβR1 inhibitor that has potential applications in immuno-oncology, inhibits TGFβR1 at an IC50 of 0.79 nM with 2000-fold selectivity against MAP4K4.
JCI Insight, 2023, e161563
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
E4432New 3,3-Dimethyl-1-butanol 3,3-Dimethyl-1-butanol (Neohexanol) is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO). 3,3-dimethyl-1-butanol negatively inhibits the signalling pathways of p65 NF-κB and  TGF-β1/Smad3. 3,3-dimethyl-1-butanol has potential applications in cardiovascular disease (CVD).
E3859 Lycopus Extract Lycopus Extract is extracted from Lycopus, which ameliorate podocytes injury by inhibiting TGF-β signaling pathway.
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.
S2234 BIBF-0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34nM.
E0769 Ginsenoside Rh4 Ginsenoside Rh4 is an important active ingredient of traditional Chinese medicine ginseng, which has been shown to inhibit Wnt/β-Catenin, JAK2/STAT3, TGF-β/Smad2/3 and other signaling pathways.
S7710 R-268712 R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
S6807 TA-02 TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2.
S7658 Kartogenin Kartogenin (KGN) is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.
Pharmaceutics, 2023, 15(7)1949
Int J Mol Sci, 2022, 24(1)390
Front Pharmacol, 2022, 13:922032
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.
Commun Biol, 2022, 5(1):750
Front Cell Dev Biol, 2021, 9:728352
Front Cell Dev Biol, 2021, 9:728352
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.
S0153 SJ000291942 SJ000291942 is a canonical bone morphogenetic proteins (BMP) signaling pathway activator.
S6654 SRI-011381 (C381) SRI-011381 (C381) 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
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.
S2308 Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.
J Transl Med, 2024, 22(1):208
Sci Rep, 2022, 12(1):7
Front Pharmacol, 2021, 12:735087
S8318 Alantolactone Alantolactone, 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
E4432New 3,3-Dimethyl-1-butanol 3,3-Dimethyl-1-butanol (Neohexanol) is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO). 3,3-dimethyl-1-butanol negatively inhibits the signalling pathways of p65 NF-κB and  TGF-β1/Smad3. 3,3-dimethyl-1-butanol has potential applications in cardiovascular disease (CVD).

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