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TGF-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
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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SB-431542
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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Pirfenidone
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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Galunisertib
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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RepSox
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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Dorsomorphin
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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Ponsegromab
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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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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LDN193189
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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Dorsomorphin dihydrochloride
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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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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SB 525334
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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Vactosertib
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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LY2109761
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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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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DMH-1
T19421206711-16-1
DMH-1 is a potent and selective Bone Morphogenetic Protein (BMP) inhibitor.
  • $53
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(E)-SIS3
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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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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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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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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SB-505124
T2462694433-59-5
SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5.
  • $34
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LDN-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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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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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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LY3200882
T51251898283-02-7
LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
  • $39
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HALOFUGINONE LACTATE
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
  • $33
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GW788388
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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LDN-214117
T19441627503-67-6
LDN-214117 is a potent and selective ALK2 inhibitor.
  • $33
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BIX02189
T24161094614-85-3
BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
  • $34
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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
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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Pentachloropseudilin
T2461269640-38-6
Pentachloropseudilin (PClP) is a reversible variant 1 myosin inhibitor with antimicrobial activity that inhibits Myo1s and class 5 myosins.Pentachloropseudilin inhibits growth factor-beta (TGF-β), which blocks host cell invasion by Trypanosoma cruzi.
  • $1,520
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LY-364947
T2048396129-53-6
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.
  • $59
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ITD-1
T22731099644-42-4
ITD-1 is a potent and highly selective TGFβ pathway inhibitor.
  • $33
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TP0427736
T24897864374-00-5
TP-0427736 is a novel potent and selective ALK5 inhibitor (IC50: 2.72 nM). P0427736 was 300-fold higher than the inhibitory effect on ALK3. TP0427736 reduces TGF-β induced growth inhibition in human outer root sheath cells and elongates the anagen phase i
  • $97
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SM1-71
T366802088179-99-9
SM1-71 is a potent multi-targeted acrylamide-modified TAK1 inhibitor that inhibits MKNK2, MAP2K1 2 3 4 6 7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A B, MAPK1 3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2.SM1-71 can be used as a kinase probe with anticancer activity and inhibits the proliferation of various cancer cell lines.
  • $44
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SRI-011381 hydrochloride
T51292070014-88-7
SRI-011381 hydrochloride, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.
  • $39
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K02288
T19141431985-92-0
K 02288 is a novel small molecule inhibitor of ALK1/2/3/6.
  • $33
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SJ000291942
T4662425613-09-8
SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway.
  • $38
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SRI-011381
T42831629138-41-5
SRI-011381, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.
  • $30
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BMS986260
T87302001559-19-7
BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
  • $48
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SJ000063181
T60644945189-68-4
SJ000063181 is a potent activator of BMP signaling, exhibiting an EC50 of ≤1 μM. It serves as a valuable chemical probe for BMP signaling analysis, owing to its ability to penetrate zebrafish embryos.
  • $44
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A 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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SD-208
T2109627536-09-8
SD-208 (ALK5 Inhibitor V), a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII.
  • $29
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Hydrochlorothiazide
T144958-93-5
Hydrochlorothiazide (HCTZ) is a Thiazide Diuretic. The physiologic effect of hydrochlorothiazide is by means of Increased Diuresis.
  • $48
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