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TGF-beta/Smad
Isoform-selective Products
Signaling Pathway
TGF-beta/Smad Products
- All (55)
- 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
| 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. |
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| 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. |
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| 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 cell testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended. |
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| 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 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! |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. | ||
| 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. |
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| S7624 | SD-208 | SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII. | ||
| 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. |
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| 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. | ||
| 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. | ||
| S7658 | Kartogenin | Kartogenin (KGN) is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S7627 | LDN-214117 | LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM. | ||
| S2308 | Hesperetin | Hesperetin is a bioflavonoid and, to be more specific, a flavanone. | ||
| 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. | ||
| 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. |
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| 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. | ||
| 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. | ||
| 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. | ||
| 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. 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. | ||
| E4798New | 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. SB 4 enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation. As an agonist of the BMP signaling pathway, SB4 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. 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| E1785New | 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. | ||
| A4012New | 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. | ||
| A4020New | 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. | ||
| 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. |
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| 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. |
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| 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 cell testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended. |
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| 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 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! |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. | ||
| 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. |
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| S7624 | SD-208 | SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII. | ||
| 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. |
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| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S7627 | LDN-214117 | LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM. | ||
| 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. | ||
| 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. | ||
| 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. 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. | ||
| E1785New | 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. TA-02 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. | ||
| 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. | ||
| 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. | ||
| A4012New | 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. | ||
| A4020New | 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. | ||
| 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. | ||
| 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.C381 physically targets the lysosome, promotes lysosomal acidification, increases breakdown of lysosomal cargo, and improves lysosome resilience to damage. | ||
| E4798New | 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. SB 4 enhances canonical BMP signaling and activates SMAD-1/5/9 phosphorylation. As an agonist of the BMP signaling pathway, SB4 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. | ||
| 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. |
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| E4798New | 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. | ||
| E1785New | 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. | ||
| A4012New | 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. | ||
| A4020New | 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. |
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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
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