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TGF-beta/Smad Inhibitors/Activators | Agonists | Antagonists | Chemicals | Modulators

Isoform-selective Products

ALK1 ALK2 ALK3 ALK4 TGFβRI/ALK5 ALK6 TGFβRII TGF-β Smad3 Smad4 Smad5 ALK7

TGF-beta/Smad Products

All (74)
TGF-beta/Smad Inhibitors (38)
TGF-beta/Smad Antibodies (8)
TGF-beta/Smad Activators (4)
TGF-beta/Smad Agonists (3)
TGF-beta/Smad Modulators (2)
New TGF-beta/Smad Products

Cat.No.	Product Name	Information	Product Use Citations
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.	Nat Biotechnol, 2025, 10.1038/s41587-025-02833-3 Signal Transduct Target Ther, 2025, 10(1):271 Cell Stem Cell, 2025, S1934-5909(25)00330-3
S7306	Dorsomorphin Dihydrochloride	Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with K_i 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.	J Clin Invest, 2025, e190215 Redox Biol, 2025, 81:103532 Redox Biol, 2025, 82:103606
S7840	Dorsomorphin	Dorsomorphin is a potent, reversible, selective AMPK inhibitor with K_i of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. This compound selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. It is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For cell testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.	Theranostics, 2025, 15(12):5931-5952 EMBO Mol Med, 2025, 17(10):2735-2761 Stem Cell Res Ther, 2025, 16(1):104
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. This compound 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 cell testing, the water-soluble S7507 LDN-193189 2HCl is recommended.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!	Cell Metab, 2025, S1550-4131(25)00334-1 Nat Commun, 2025, 16(1):4432 Theranostics, 2025, 15(14):7127-7153
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.	Signal Transduct Target Ther, 2025, 10(1):257 Exp Mol Med, 2025, 57(6):1324-1338 Biochem Pharmacol, 2025, 240:117082
S2704	LY2109761	LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with K_i of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. This compound blocks autophagy and induces apoptosis.	J Tissue Eng, 2025, 16:20417314251376104 Cancer Metab, 2025, 13(1):3 iScience, 2025, 28(2):111756
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.	J Control Release, 2025, S0168-3659(25)00029-X Commun Biol, 2025, 8(1):152 Sci Rep, 2025, 15(1):25926
S7507	LDN-193189 Dihydrochloride	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.	Nat Commun, 2025, 16(1):5543 Adv Sci (Weinh), 2025, 12(2):e2406509 Adv Healthc Mater, 2025, e04817.
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, 2025, 21(13):5922-5935 EMBO Rep, 2025, 26(12):3162-3186 Commun Biol, 2025, 8(1):471
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.	Cell, 2025, S0092-8674(25)00807-4 Cell Metab, 2025, S1550-4131(25)00334-1 Trends Biotechnol, 2025, 43(8):2029-2048
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 Commun Signal, 2024, 22(1):242
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. This compound attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.	Biomed Pharmacother, 2025, 188:118216 Eur Respir J, 2024, 2300580 Phytomedicine, 2024, 135:156051
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. This compound inhibits autophagy.	Cell Stem Cell, 2025, S1934-5909(25)00081-5 J Adv Res, 2025, S2090-1232(25)00553-3 Commun Biol, 2025, 8(1):1177
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.	Cell Rep, 2025, 44(5):115675 Calcif Tissue Int, 2025, 116(1):57 Heliyon, 2024, 10(20):e39475
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.	Mol Carcinog, 2024, 10.1002/mc.23715 J Biol Chem, 2023, 299(4):103017 proquest, 2023,
S7692	A-83-01	A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. This compound 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.	Cell, 2025, S0092-8674(25)00807-4 Nat Genet, 2025, 57(1):165-179 Nat Genet, 2025, 57(1):165-179
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 Nat Commun, 2022, 13(1):2844
S7624	SD-208	SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.	J Cancer, 2024, 15(9):2448-2459 JCI Insight, 2023, 8(3)e166688 Cancers (Basel), 2023, 10.3390/cancers15205086
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.	Nat Commun, 2024, 15(1):7388 Cells, 2024, 13(10)879 Cells, 2024, 13(10)879
S1576	Sulfasalazine	Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. This compound is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. It induces ferroptosis, apoptosis and autophagy.	Med Oncol, 2024, 41(8):188 Adv Sci (Weinh), 2023, 10(20):e2300517 Proc Natl Acad Sci U S A, 2022, 119(36):e2117396119
S3552	SIS3	SIS3 is a cell-permeable inhibitor of Smad3 that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling. This compound reduces TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.	J Virol, 2025, 99(9):e0043525 Life Sci Alliance, 2024, 7(6)e202302408 Front Bioeng Biotechnol, 2023, 11:1281157
S7658	Kartogenin	Kartogenin (KGN) is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.	Sci Rep, 2024, 14(1):15022 Pharmaceutics, 2023, 15(7)1949 Int J Mol Sci, 2022, 24(1)390
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.	World J Gastrointest Oncol, 2025, 17(1):97831 Redox Biol, 2024, 76:103349 Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00989-9
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.	Sci Adv, 2025, 11(28):eadw1883 Cell Rep, 2024, 43(9):114728 J Neurochem, 2024, 10.1111/jnc.16102
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.	EMBO Rep, 2024, 25(7):3090-3115 Am J Pathol, 2023, S0002-9440(23)00047-0 Am J Pathol, 2023, 193(5):532-547
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. This compound 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.C381 physically targets the lysosome, promotes lysosomal acidification, increases breakdown of lysosomal cargo, and improves lysosome resilience to damage.	Noncoding RNA Res, 2025, 13:1-14 SLAS Technol, 2024, 29(5):100190 Dis Model Mech, 2022, dmm.046979
S7627	LDN-214117	LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.	Cancer Res, 2024, 10.1158/0008-5472.CAN-23-2631 bioRxiv, 2023, 2023.06.14.544941 FASEB J, 2021, 35(3):e21263
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.	iScience, 2025, 28(3):112015 Front Cell Dev Biol, 2025, 13:1513163 Cell Regen, 2025, 14(1):18
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.	Molecules, 2024, 29(8)1866 Molecules, 2024, 29(8)1866 Nat Commun, 2022, 13(1):107
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.	Nutrients, 2024, 16(17)2991 JCI Insight, 2023, e161563
A2113	Anti-human/mouse TGF-β-InVivo	The 1D11.16.8 monoclonal antibody reacts with mouse, human, rat, monkey, hamster, canine and bovine TGF-β (transforming growth factor beta) isoforms 1, 2 and 3.The 1D11.16.8 monoclonal antibody is a neutralizing antibody.	Cells, 2024, 13(10)879 Cells, 2024, 13(10)879 Cell Discov, 2023, 9(1):28
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.	J Dairy Sci, 2025, S0022-0302(25)00833-1 PLoS One, 2021, 16(5):e0252541
F1624	TGF β1 Antibody [P22B16]	TGF beta 1,Transforming Growth Factor-beta1	Cell Death Dis, 2025, 16(1):597
F0363	Smad2/3 Antibody [M18H19]	Mothers against decapentaplegic homolog 3, MAD homolog 3, Mothers against DPP homolog 3, Mad3, JV15-2, SMAD 3, Smad3, hSMAD3, hMAD-3, MADH3, SMAD family member 3, Mothers against decapentaplegic homolog 2, MAD homolog 2, JV18-1, hMAD-2, SMAD 2, Smad2, hSMAD2, Mothers against DPP homolog 2, Mad-related protein 2, SMAD family member 2	Cell Death Dis, 2025, 16(1):597
F0364	Smad3 Antibody [J9N13]
F1360	TGF-β Receptor III Antibody [M9F17]	TGF beta Receptor III/TGFBR3,TGF-beta Receptor III
F1016	TGFBI Antibody [P17H24]	TGFBI,βIG-H3
F0309	Smad2 Antibody [E24M24]
F1689^New	Phospho-Smad2 (Ser255) Antibody [H13B7]		J Plast Surg Hand Surg, 2021, 55(5):284-293.
F0347	Phospho-Smad1/5/9 (S463/465, S463/465, S465/467) Antibody [L11J17]	Phospho-Smad1 (Ser463/465)/ Smad5 (Ser463/465)/ Smad9 (Ser465/467),SMAD1 + SMAD5 + SMAD9 (phospho S463 + S465 + S467)
F0308	Smad1 Antibody [N8K18]
F0976	BMP4 Antibody [J12D21]	BMP4 Rabbit mAb recognizes endogenous levels of total BMP4 protein.	Cancer Metab, 2023, 11(1):9
F1052	Smad5 Antibody [A13M1]	Mothers against decapentaplegic homolog 5, MAD homolog 5, Mothers against DPP homolog 5, JV5-1, SMAD family member 5, SMAD 5, Smad5, hSmad5, MADH5	Cancer Metab, 2023, 11(1):9 Am J Cancer Res, 2021, 11(3):793-811
F2875^New	Phospho-Smad1/5/9 (S463/465/467) Antibody [K12G16]	Phospho-Smad1 (Ser463/465)/ Smad5 (Ser463/465)/ Smad9 (Ser465/467),SMAD1 + SMAD5 + SMAD9 (phospho S463 + S465 + S467)
A2370	Elezanumab (Anti-RGMA)	Elezanumab (Anti-RGMA) is a human monoclonal antibody that selectively targets repulsive guidance molecule A (RGMa). Elezanumab potently inhibited RGMa mediated BMP signalling via the SMAD1/5/8 pathway with IC50 of 97 pM. MW: 146.44 kD.
S3223	L-Quebrachitol	L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation and cell DNA synthesis. This compound 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.
E4798^New	SRI-011381 hydrochloride	SRI-011381 hydrochloride is an agonist of the transforming growth factor-beta (TGF-β) signalling pathway and exhibits neuroprotective effects with the potential to treat Alzheimer's disease. It also increases fibronectin expression in the NIH‐3T3 cells stimulated by metformin.
E4432	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. This compound enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation. As an agonist of the BMP signaling pathway, this chemical can significantly upregulate the expression levels of classical BMP4 downstream target genes (such as DNA binding inhibitors Id1 and Id3).
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. This compound has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. It downregulates Smad3 and p38 signaling pathways.
A2422	Garetosmab (Anti-INHBA / Activin A)	Garetosmab (Anti-INHBA / Activin A) is a fully human IgG4 monoclonal antibody that specifically inhibits activin A. Garetosmab can be used for fibrodysplasia ossificans progressiva (FOP) research. MW: 145.5 kD.	Nat Commun, 2025, 16(1):6577
F3338^New	Smad1 Antibody [K19G18]
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.
F2846^New	Phospho-Smad3 (Ser423/Ser425) Antibody [L3N2]	Phospho-Smad3 (Ser423/425),Smad3 (phospho S423 + S425), Smad5 (463/465), Smad1 (Ser 463/465), Smad2 (Ser 465/467)d5 (Se
F2576^New	GDNF Antibody [M11F22]
A2694	Anti-TGFb1 (SRK181)	Anti-TGFb1 (SRK181) is a monoclonal antibody directed against latent human transforming growth factor (TGF)-beta 1 with potential antineoplastic activity. MW : 150 kD.
A2695	Anti-TGFb1 (M7824)	Anti-TGFb1 (M7824) is a bifunctional monoclonal antibody targeting programmed death ligand 1 (PD-L1) and transforming growth factor beta 1 (TGFb1). It exhibits anti-tumor efficacy against breast and colon carcinomas.
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.	Kidney360, 2025, 10.34067/KID.0000000852
E1785	PF-06952229	PF-06952229(UNII-1KKS7U3X86) is a selective, orally available inhibitor of the serine/threonine kinase TGF-β receptor 1 (TGF-β-R1). It inhibits pSMAD2 in both tumor and immune cells, reducing TGF-β signalling and reversing EMT in vitro. It modulates the tumor immune microenvironment and shows antitumor activity in mouse models.
A4012^New	Tqb2858 (Anti-PD-L1 & TGF-β)	Tqb2858 is a bifunctional fusion protein consisting of a monoclonal antibody targeting programmed death ligand 1 (PD-L1) fused with the extracellular domain of the transforming growth factor beta (TGF-β) receptor. It simultaneously neutralizes TGF-β on tumor cells and inhibits PD-L1 activity, exhibiting potential antineoplastic and immune checkpoint-modulating effects. MW: 178.22 KD.
F2633^New	Phospho-Smad1 (Ser206) Antibody [D10B24]
A4020^New	Abt-122 (Anti-IL-17 & TNF-alpha)	Abt-122 is a dual variable domain immunoglobulin (DVD-Ig) that targets human TNF and IL-17A, with the potential to treat rheumatoid arthritis (RA). MW: 198.74 KD.
F0031^New	Nestin Antibody [M9J9]	Nestin,Nestin, Human
F2851^New	Smad3 Antibody [H20E2]
F3678^New	SARA Antibody [N8F11]	SARA
A2336	Fresolimumab (Anti-TGFb1)	Fresolimumab (Anti-TGFb1) is a pan-specific, recombinant, fully human monoclonal antibody directed against human transforming growth factor (TGF) beta 1, 2, and 3 with potential antineoplastic activity. MW : 145.5 KD.
S6807	TA-02	TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. This compound 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.	Nat Biotechnol, 2025, 10.1038/s41587-025-02833-3 Signal Transduct Target Ther, 2025, 10(1):271 Cell Stem Cell, 2025, S1934-5909(25)00330-3
S7306	Dorsomorphin Dihydrochloride	Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with K_i 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.	J Clin Invest, 2025, e190215 Redox Biol, 2025, 81:103532 Redox Biol, 2025, 82:103606
S7840	Dorsomorphin	Dorsomorphin is a potent, reversible, selective AMPK inhibitor with K_i of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. This compound selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. It is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For cell testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.	Theranostics, 2025, 15(12):5931-5952 EMBO Mol Med, 2025, 17(10):2735-2761 Stem Cell Res Ther, 2025, 16(1):104
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. This compound 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 cell testing, the water-soluble S7507 LDN-193189 2HCl is recommended.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!	Cell Metab, 2025, S1550-4131(25)00334-1 Nat Commun, 2025, 16(1):4432 Theranostics, 2025, 15(14):7127-7153
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.	Signal Transduct Target Ther, 2025, 10(1):257 Exp Mol Med, 2025, 57(6):1324-1338 Biochem Pharmacol, 2025, 240:117082
S2704	LY2109761	LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with K_i of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. This compound blocks autophagy and induces apoptosis.	J Tissue Eng, 2025, 16:20417314251376104 Cancer Metab, 2025, 13(1):3 iScience, 2025, 28(2):111756
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.	J Control Release, 2025, S0168-3659(25)00029-X Commun Biol, 2025, 8(1):152 Sci Rep, 2025, 15(1):25926
S7507	LDN-193189 Dihydrochloride	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.	Nat Commun, 2025, 16(1):5543 Adv Sci (Weinh), 2025, 12(2):e2406509 Adv Healthc Mater, 2025, e04817.
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, 2025, 21(13):5922-5935 EMBO Rep, 2025, 26(12):3162-3186 Commun Biol, 2025, 8(1):471
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.	Cell, 2025, S0092-8674(25)00807-4 Cell Metab, 2025, S1550-4131(25)00334-1 Trends Biotechnol, 2025, 43(8):2029-2048
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 Commun Signal, 2024, 22(1):242
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. This compound attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.	Biomed Pharmacother, 2025, 188:118216 Eur Respir J, 2024, 2300580 Phytomedicine, 2024, 135:156051
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. This compound inhibits autophagy.	Cell Stem Cell, 2025, S1934-5909(25)00081-5 J Adv Res, 2025, S2090-1232(25)00553-3 Commun Biol, 2025, 8(1):1177
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.	Cell Rep, 2025, 44(5):115675 Calcif Tissue Int, 2025, 116(1):57 Heliyon, 2024, 10(20):e39475
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.	Mol Carcinog, 2024, 10.1002/mc.23715 J Biol Chem, 2023, 299(4):103017 proquest, 2023,
S7692	A-83-01	A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. This compound 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.	Cell, 2025, S0092-8674(25)00807-4 Nat Genet, 2025, 57(1):165-179 Nat Genet, 2025, 57(1):165-179
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 Nat Commun, 2022, 13(1):2844
S7624	SD-208	SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.	J Cancer, 2024, 15(9):2448-2459 JCI Insight, 2023, 8(3)e166688 Cancers (Basel), 2023, 10.3390/cancers15205086
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.	Nat Commun, 2024, 15(1):7388 Cells, 2024, 13(10)879 Cells, 2024, 13(10)879
S1576	Sulfasalazine	Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. This compound is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. It induces ferroptosis, apoptosis and autophagy.	Med Oncol, 2024, 41(8):188 Adv Sci (Weinh), 2023, 10(20):e2300517 Proc Natl Acad Sci U S A, 2022, 119(36):e2117396119
S3552	SIS3	SIS3 is a cell-permeable inhibitor of Smad3 that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling. This compound reduces TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.	J Virol, 2025, 99(9):e0043525 Life Sci Alliance, 2024, 7(6)e202302408 Front Bioeng Biotechnol, 2023, 11:1281157
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.	World J Gastrointest Oncol, 2025, 17(1):97831 Redox Biol, 2024, 76:103349 Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00989-9
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.	Sci Adv, 2025, 11(28):eadw1883 Cell Rep, 2024, 43(9):114728 J Neurochem, 2024, 10.1111/jnc.16102
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.	EMBO Rep, 2024, 25(7):3090-3115 Am J Pathol, 2023, S0002-9440(23)00047-0 Am J Pathol, 2023, 193(5):532-547
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. This compound 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.	Cancer Res, 2024, 10.1158/0008-5472.CAN-23-2631 bioRxiv, 2023, 2023.06.14.544941 FASEB J, 2021, 35(3):e21263
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.	Nutrients, 2024, 16(17)2991 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.	J Dairy Sci, 2025, S0022-0302(25)00833-1 PLoS One, 2021, 16(5):e0252541
E4432	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. This compound has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. It 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.	Kidney360, 2025, 10.34067/KID.0000000852
E1785	PF-06952229	PF-06952229(UNII-1KKS7U3X86) is a selective, orally available inhibitor of the serine/threonine kinase TGF-β receptor 1 (TGF-β-R1). It inhibits pSMAD2 in both tumor and immune cells, reducing TGF-β signalling and reversing EMT in vitro. It modulates the tumor immune microenvironment and shows antitumor activity in mouse models.
S6807	TA-02	TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. This compound especially inhibits TGFBR-2.
A2113	Anti-human/mouse TGF-β-InVivo	The 1D11.16.8 monoclonal antibody reacts with mouse, human, rat, monkey, hamster, canine and bovine TGF-β (transforming growth factor beta) isoforms 1, 2 and 3.The 1D11.16.8 monoclonal antibody is a neutralizing antibody.	Cells, 2024, 13(10)879 Cells, 2024, 13(10)879 Cell Discov, 2023, 9(1):28
A2370	Elezanumab (Anti-RGMA)	Elezanumab (Anti-RGMA) is a human monoclonal antibody that selectively targets repulsive guidance molecule A (RGMa). Elezanumab potently inhibited RGMa mediated BMP signalling via the SMAD1/5/8 pathway with IC50 of 97 pM. MW: 146.44 kD.
A2422	Garetosmab (Anti-INHBA / Activin A)	Garetosmab (Anti-INHBA / Activin A) is a fully human IgG4 monoclonal antibody that specifically inhibits activin A. Garetosmab can be used for fibrodysplasia ossificans progressiva (FOP) research. MW: 145.5 kD.	Nat Commun, 2025, 16(1):6577
A2694	Anti-TGFb1 (SRK181)	Anti-TGFb1 (SRK181) is a monoclonal antibody directed against latent human transforming growth factor (TGF)-beta 1 with potential antineoplastic activity. MW : 150 kD.
A2695	Anti-TGFb1 (M7824)	Anti-TGFb1 (M7824) is a bifunctional monoclonal antibody targeting programmed death ligand 1 (PD-L1) and transforming growth factor beta 1 (TGFb1). It exhibits anti-tumor efficacy against breast and colon carcinomas.
A4012^New	Tqb2858 (Anti-PD-L1 & TGF-β)	Tqb2858 is a bifunctional fusion protein consisting of a monoclonal antibody targeting programmed death ligand 1 (PD-L1) fused with the extracellular domain of the transforming growth factor beta (TGF-β) receptor. It simultaneously neutralizes TGF-β on tumor cells and inhibits PD-L1 activity, exhibiting potential antineoplastic and immune checkpoint-modulating effects. MW: 178.22 KD.
A4020^New	Abt-122 (Anti-IL-17 & TNF-alpha)	Abt-122 is a dual variable domain immunoglobulin (DVD-Ig) that targets human TNF and IL-17A, with the potential to treat rheumatoid arthritis (RA). MW: 198.74 KD.
A2336	Fresolimumab (Anti-TGFb1)	Fresolimumab (Anti-TGFb1) is a pan-specific, recombinant, fully human monoclonal antibody directed against human transforming growth factor (TGF) beta 1, 2, and 3 with potential antineoplastic activity. MW : 145.5 KD.
S7658	Kartogenin	Kartogenin (KGN) is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.	Sci Rep, 2024, 14(1):15022 Pharmaceutics, 2023, 15(7)1949 Int J Mol Sci, 2022, 24(1)390
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.	iScience, 2025, 28(3):112015 Front Cell Dev Biol, 2025, 13:1513163 Cell Regen, 2025, 14(1):18
S3223	L-Quebrachitol	L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation and cell DNA synthesis. This compound 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.C381 physically targets the lysosome, promotes lysosomal acidification, increases breakdown of lysosomal cargo, and improves lysosome resilience to damage.	Noncoding RNA Res, 2025, 13:1-14 SLAS Technol, 2024, 29(5):100190 Dis Model Mech, 2022, dmm.046979
E4798^New	SRI-011381 hydrochloride	SRI-011381 hydrochloride is an agonist of the transforming growth factor-beta (TGF-β) signalling pathway and exhibits neuroprotective effects with the potential to treat Alzheimer's disease. It also increases fibronectin expression in the NIH‐3T3 cells stimulated by metformin.
S0523	SB 4	SB 4 is a potent and selective agonist of bone morphogenetic protein 4 (BMP4) signaling with EC50 of 74 nM. This compound enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation. As an agonist of the BMP signaling pathway, this chemical can significantly upregulate the expression levels of classical BMP4 downstream target genes (such as DNA binding inhibitors Id1 and Id3).
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.	Molecules, 2024, 29(8)1866 Molecules, 2024, 29(8)1866 Nat Commun, 2022, 13(1):107
F1689^New	Phospho-Smad2 (Ser255) Antibody [H13B7]		J Plast Surg Hand Surg, 2021, 55(5):284-293.
F2875^New	Phospho-Smad1/5/9 (S463/465/467) Antibody [K12G16]	Phospho-Smad1 (Ser463/465)/ Smad5 (Ser463/465)/ Smad9 (Ser465/467),SMAD1 + SMAD5 + SMAD9 (phospho S463 + S465 + S467)
E4798^New	SRI-011381 hydrochloride	SRI-011381 hydrochloride is an agonist of the transforming growth factor-beta (TGF-β) signalling pathway and exhibits neuroprotective effects with the potential to treat Alzheimer's disease. It also increases fibronectin expression in the NIH‐3T3 cells stimulated by metformin.
F3338^New	Smad1 Antibody [K19G18]
F2846^New	Phospho-Smad3 (Ser423/Ser425) Antibody [L3N2]	Phospho-Smad3 (Ser423/425),Smad3 (phospho S423 + S425), Smad5 (463/465), Smad1 (Ser 463/465), Smad2 (Ser 465/467)d5 (Se
F2576^New	GDNF Antibody [M11F22]
A4012^New	Tqb2858 (Anti-PD-L1 & TGF-β)	Tqb2858 is a bifunctional fusion protein consisting of a monoclonal antibody targeting programmed death ligand 1 (PD-L1) fused with the extracellular domain of the transforming growth factor beta (TGF-β) receptor. It simultaneously neutralizes TGF-β on tumor cells and inhibits PD-L1 activity, exhibiting potential antineoplastic and immune checkpoint-modulating effects. MW: 178.22 KD.
F2633^New	Phospho-Smad1 (Ser206) Antibody [D10B24]
A4020^New	Abt-122 (Anti-IL-17 & TNF-alpha)	Abt-122 is a dual variable domain immunoglobulin (DVD-Ig) that targets human TNF and IL-17A, with the potential to treat rheumatoid arthritis (RA). MW: 198.74 KD.
F0031^New	Nestin Antibody [M9J9]	Nestin,Nestin, Human
F2851^New	Smad3 Antibody [H20E2]
F3678^New	SARA Antibody [N8F11]	SARA

TGF-beta/Smad Inhibitors/Activators | Agonists | Antagonists | Chemicals | Modulators

Isoform-selective Products

TGF-beta/Smad Products

Signaling Pathway Map