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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.
SB-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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CitedA 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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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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CitedDorsomorphin 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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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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CitedChebulinic 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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Monocrotaline 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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CitedLDN193189 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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CitedCarotuximab
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.
- $129
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Dorsomorphin 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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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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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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CitedFresolimumab
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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SB 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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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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Kartogenin
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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R-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
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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(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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CitedAstragaloside 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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Disitertide 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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DMH-1 Cited
T19421206711-16-1
DMH-1 is a potent and selective Bone Morphogenetic Protein (BMP) inhibitor.
- $53
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