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Stem CellsTGF-beta/Smad
The transforming growth factor beta (TGFB) signaling pathway is involved in many cellular processes in both the adult organism and the developing embryo including cell growth, cell differentiation, apoptosis, cellular homeostasis and other cellular functions. In spite of the wide range of cellular processes that the TGFβ signaling pathway regulates, the process is relatively simple. TGFβ superfamily ligands bind to a type II receptor, which recruits and phosphorylates a type I receptor. The type I receptor then phosphorylates receptor-regulated SMADs (R-SMADs) which can now bind the coSMAD SMAD4. R-SMAD/coSMAD complexes accumulate in the nucleus where they act as transcription factors and participate in the regulation of target gene expression.
A 83-01
Cited
T3031909910-43-6
A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12 45 7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.
- $52
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CitedSB-431542 Cited
T1726301836-41-9
SB-431542 is an inhibitor of ALK5 TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.
- $50
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CitedPirfenidone Cited
T238653179-13-8
Pirfenidone (AMR69) inhibits the production of CCL2 and CCL12 in fibroblasts and also decreases TGF-β2 protein levels. Pirfenidone is an antifibrotic agent that is commonly used in studies related to pulmonary fibrosis and also has anti-inflammatory activity.
- $30
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CitedGalunisertib Cited
T2510700874-72-2
Galunisertib (LY2157299) is a TGF-β receptor type I (TGF-βRI) inhibitor (IC50=56 nM) that is selective. Galunisertib has antitumor activity and can be used in combination with PD-1 inhibitors.
- $40
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CitedRepSox Cited
T6337446859-33-2
RepSox (ALK5 Inhibitor II) is a TGFβR-1 ALK5 inhibitor that selectively inhibits the binding of ATP to ALK5 and the autophosphorylation of ALK5 (IC50=23 4 nM). RepSox induces adipogenesis in MEFs cells.
- $30
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CitedPonsegromab
T767742368950-15-4
Ponsegromab (PF 06946860) is a selective and effective humanized anti-GDF15 antibody inhibitor with anti-cachexic activity. It binds to GDF15, preventing its interaction with GFRAL and disrupting GDF15 GFRAL mediated signaling. Ponsegromab has potential anticancer activity and can be used to treat cancer patients with cancer anorexia cachexia syndrome.
- $297
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Dorsomorphin
Cited
T1977866405-64-3
Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity.
- $48
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CitedSkullcapflavone II
TN104055084-08-7
Skullcapflavone II is a flavonoid derived from Scutellaria baicalensis, a widely used herbal medicine in anti-inflammatory and anticancer therapy. Skullcapflavone II may have therapeutic potential for the treatment of allergic asthma.Skullcapflavone II regulates osteoclast differentiation, survival, and function. Skullcapflavone II exerts potent antimicrobial activity against M. aurum and M. bovis BCG
- $98
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Carotuximab
T769411268714-50-6
Carotuximab (DE-122) is a novel endocholine antibody with strong antiangiogenic and anti-inflammatory activity. Carotuximab blocks endothelial glycoprotein (CD105) and its downstream Smad signaling pathway. Carotuximab has immunomodulatory and antitumor effects to prevent human endothelial dysfunction induced by hypercholesterolemia and hyperglycemia.
- $247
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PF-06952229
T124331801333-55-0In house
PF-06952229 is a selective inhibitor of TGFβRI. PF-06952229 can be used in studies about the treatment of solid tumors, specifically metastatic breast cancer.
- $113
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Chebulinic acid
TQ018418942-26-2
Chebulinic acid is a potent inhibitor of M. tuberculosis DNA gyrase. It also can inhibit SMAD-3 phosphorylation and H+ K+-ATPase activity.
- $67
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LDN193189 Cited
T19351062368-24-4
LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8 0.8 5.3 16.7 nM for ALK1 2 3 6).
- $41
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CitedMonocrotaline Cited
T2803315-22-0
Monocrotaline (Crotaline) is a pyrrolizidine alkaloid extracted from the seeds of the Crotalaria plant. Monocrotaline has certain cellular activity against HepG2 cells and can induce pulmonary hypertension in rodents.
- $41
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CitedDorsomorphin dihydrochloride Cited
T61461219168-18-9
Dorsomorphin dihydrochloride (BML-275 2HCl) is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.
- $30
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CitedHydroxysafflor yellow A Cited
T367478281-02-4
Hydroxysafflor yellow A (Safflomin A) inhibits adipogenesis by increasing HSL promoter activities, effectively protects the liver from long-term alcohol injury by enhancing antioxidant capacity and inhibiting the expression of TGF-β, prevents steroid-induced avascular necrosis of the femoral head by inhibiting primary bone marrow-derived mesenchymal stromal cells, and exhibits anti-tumor effects.
- $70
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CitedR-268712
T16708879487-87-3
R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor.
- $39
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Halofuginone hydrobromide Cited
T352464924-67-0
Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.
- $31
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CitedSB 525334 Cited
T1763356559-20-1
SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM).
- $32
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CitedKartogenin
T17484727-31-5
Kartogenin (KGN) is an activator of the smad4 smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.
- $30
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LY2109761 Cited
T2123700874-71-1
LY2109761 is a novel selective TGF-β receptor type I II (TβRI II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2.
- $39
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CitedDMH-1 Cited
T19421206711-16-1
DMH-1 is a potent and selective Bone Morphogenetic Protein (BMP) inhibitor.
- $53
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Cited(E)-SIS3 Cited
T3636521984-48-5
(E)-SIS3 (SIS3), a selective Smad3 inhibitor, can attenuate TGF-β1-dependent Smad3 phosphorylation and DNA binding. It has no effect on p38 MAPK, Smad2, ERK or PI3K signaling. It also inhibits TGF-β1-induced myofibroblast differentiation of dermal fibroblasts and inhibits TGF-β2-induced endothelial cell differentiation in iPSCs.
- $36
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CitedDisitertide acetate
T11052L
Disitertide acetate (P144 acetate) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide acetate is also a PI3K inhibitor and an apoptosis inducer.
- $152
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Ascrinvacumab
T768581463459-96-2
Ascrinvacumab (PF-03446962) is a highly humanized IgG2 monoclonal antibody against ALK-1 with a Kd value of 7 nM for human ALK1. It has an inhibitory effect on TGF-β and can be used to study hepatocellular carcinoma (HCC).
- $247
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Tubastatin
T290231239034-70-8
Tubastatin inhibits TGF-β1-induced phosphorylation of S6K, HIF-1α expression and VEG F expression.Tubastatin inhibits TGF-β1-induced inhibition of LC3B-II, a marker of autophagosome formation.
- $40
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AXL-IN-13
T733002376928-82-2In house
AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 of 1.6 nM and a Kd of 0.26 nM. It exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion.
- $79
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Vactosertib Cited
T64961352608-82-2
Vactosertib (EW-7197) is an orally bioavailable inhibitor of the serine threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity.
- $39
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CitedHalofuginone
T685655837-20-2
Halofuginone (RU-19110), the competitive inhibitor of prolyl-tRNA synthetase(Ki=18.3 nM), could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng ml in the mammal.
- $31
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Fresolimumab
T76681948564-73-6
Fresolimumab (GC1008) is a specific human anti-transforming growth factor β monoclonal antibody that binds to the active forms of human TGFβ1, TGFβ2, and TGFβ3 and can be used to study focal segmental glomerulosclerosis and cancer in adults.
- $597
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Asiaticoside
T302516830-15-2
Asiaticoside (Emdecassol) (Madecassol) is the active chemical component of the plant Centella asiatica. Asiaticoside is used to study potential treatments for wounds and burns.
- $50
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SB-505124 Cited
T2462694433-59-5
SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5.
- $34
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CitedHesperetin Cited
T2565520-33-2
Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.
- $38
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CitedLY3200882
T51251898283-02-7
LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
- $39
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LSKL TFA
TP2147
LSKL TFA (H-Leu-Ser-Lys-Leu-NH2 TFA) is a LAP-TGFβ derivative and a TGF-β1 antagonist that can cross the blood-brain barrier, inhibits the binding of TSP-1 to LAP and reduces renal interstitial fibrosis and liver fibrosis, inhibits subarachnoid fibrosis by inhibiting TSP-1-mediated TGF-β1 activity, prevents the occurrence of chronic hydrocephalus and improves long-term neurocognitive deficits after subarachnoid hemorrhage.
- $38
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Astragaloside II
T392484676-89-1
Astragaloside II (Astrasieversianin VIII) is an effective MDR reversal agent and may be a potential adjunctive agent for hepatic cancer chemotherapy. Astragaloside II also induces osteogenic activities, differentiation, proliferation, and mineralization, through the bone morphogenetic protein-2 MAPK and Smad1 5 8 pathways.
- $34
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Alantolactone Cited
T2896546-43-0
Alantolactone is a selective inhibitor of STAT3 that induces cancer-associated apoptosis and has antitumor activity.
- $50
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CitedA 77-01
T2098607737-87-1
A 77-01 is a potent inhibitor of the TGF-(beta) type I receptor superfamily activin-like kinase ALK5, with an IC50 of 25 nM.
- $41
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EW-7195
T387521352609-28-9
EW-7195 is a selective and potent inhibitor of ALK5 (TGFβR1) with an IC50 value of 4.83 nM.EW-7195 has an affinity for ALK5 that is more than 300-fold higher than that of p38α.EW-7195 has an inhibitory effect on TGF-β1-induced Smad signaling, epithelial mesenchymal transition (EMT), and breast cancer metastasis to the lungs.
- $133
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HALOFUGINONE LACTATE Cited
T878582186-71-8
HALOFUGINONE LACTATE is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity
- $55
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CitedLDN-193189 2HCl
T353481435934-00-1
LDN-193189 2HCl (DM-3189 2HCl) is a selective BMP signaling inhibitor that inhibits ALK1,ALK2,ALK3 and ALK6, showing IC50s of 0.8 nM, 0.8 nM, 5.3 nM, and 16.7 nM, respectively, in kinase assays.LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively. LDN-193189 2HCl inhibited the transcriptional activity of BMP type I receptors ALK2 and ALK3 in C2C12 cells, with IC50s of 5 nM and 30 nM, respectively, and was 200-fold more selective for BMP than for TGF-β.
- $67
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Oxymatrine Cited
T275416837-52-8
Oxymatrine (Oxysophoridine) is an alkaloid isolated from Sophora flavescens, used as the antibiotic. It is a traditional Chinese medicine used in the treatment against hepatitis B virus.It can also inhibit iNOS expression and TGF - β Smad pathway.
- $41
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CitedGW788388
T1800452342-67-5
GW788388 is a potent and selective inhibitor of ALK5, and it also inhibits TGF-(beta) type II receptor and activin type II receptor activities.
- $58
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Trimethylamine N-oxide
T412451184-78-7
Trimethylamine N-oxide (TMAO) is a colorless amine oxide produced from choline, betaine, and carnitine via intestinal microbial metabolism that accumulates in tissues of marine animals and prevents the protein-damaging effects of urea.Trimethylamine N-oxide induces inflammation through activation of ROS NLRP3 inflammasomes, which can induce fibroblast differentiation and cardiac fibrosis.
- $29
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BIX02189 Cited
T24161094614-85-3
BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
- $34
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CitedGaretosmab
T770192097125-54-5
Garetosmab (REGN 2477) is A whole-human IgG4 monoclonal antibody that selectively inhibits activin A and acts on COVID-19 44. Garetosmab has potential anti-cancer activity and can be used to study ossifying fibrous dysplasia (FOP) and cancer.
- $328
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TGFβ1-IN-1
T613892348795-14-0
TGFβ1-IN-1 is an orally active TGF-β1 inhibitor that inhibits the production of TGF-β1-induced fibrotic markers (α-SMA and fibronectin) and can be used for the study of cancer and autoimmune diseases.
- $92
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BMP signaling agonist sb4 Cited
T7799100874-08-6
BMP signaling agonist sb4 (SB 4) is an agonist of benzoxazole bone morphogenetic protein (BMP) signaling (EC50 :74 nM)
- $39
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