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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.
カタログ番号 製品名
T12923 SIS3 free base SIS3 free base is a potent and selective Smad3 phosphorylation inhibitor. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
T7377 LSKL, Inhibitor of Thrombospondin (TSP-1) LSKL, Inhibitor of Thrombospondin (TSP-1) is a peptide derived from the latency-associated peptide, inhibits thrombospondin (TSP-1) activation of TGF-β.
T35348 LDN-193189 2HCl
TN3753 Dalbergioidin Dalbergioidin exhibits tyrosinase inhibitory activity with an IC50 of 20 mM. It shows a melanin biosynthesis inhibition zone in the culture plate of Streptomyces...
T13137 TGFβRI-IN-1 TGFβRI-IN-1 is an oral active and selective inhibitor of TGFβ receptor type I (TGFβRI) kinase(IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively...
T61301 Chromenone 1 Chromenone 1 is a potent potentiator of osteogenic bone morphogenetic protein (BMP). Chromenone 1 induces a pronounced, kinase-independent, negative TGFβ feedbac...
T20319 Pentabromophenol Pentabromophenol inhibits TGF-β signaling by accelerating the degradation of type II TGF-β receptors via caveolae-mediated endocytosis.
T24897 TP0427736 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...
T9523 TGFβRI-IN-3 TGFβRI-IN-3 inhibits TGFβR1 with an IC 50 of 0.79 nM with 2000-fold selectivity against MAP4K4. TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor that has poten...
T12433 PF-06952229 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.
T7676 LSKL, Inhibitor of Thrombospondin TSP-1 acetate LSKL, Inhibitor of Thrombospondin TSP-1 acetate is activation of TGF-β .
T11052L Disitertide acetate Disitertide acetate is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitert...
T1748 Kartogenin Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.
T3524 Halofuginone hydrobromide Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of...
T6856 Halofuginone Halofuginone, 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 mamm...
T3031 A 83-01 A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 with IC50 values of 12 n...
T2109 SD-208 SD-208, a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII.
T1800 GW788388 GW788388 is a potent and selective inhibitor of ALK5, also inhibits TGF-(beta) type II receptor and activin type II receptor activities.
T8730 BMS986260 BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
T2565 Hesperetin Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges....
T6337 RepSox RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor.
T3636 (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 signali...
TQ0184 Chebulinic acid Chebulinic acid is a potent inhibitor of M. tuberculosis DNA gyrase. It also can inhibit SMAD-3 phosphorylation and H+ K+-ATPase activity.
T1935 LDN193189 LDN193189 (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)....
T4283 SRI-011381 SRI-011381, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.
T6324 BIX02188 BIX02188 is a specific MEK5 inhibitor (IC50: 4.3 nM), also inhibits ERK5 catalytic activity (IC50: 810 nM), and does not inhibit closely related kinases MEK1/2, ...
T4662 SJ000291942 SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway.
T1900 LDN-212854 LDN-212854, a novel BMP inhibitor, exhibits greater selectivity for BMP versus the TGF-β type I receptors; possesses differences towards ALK2(IC50=1.3 nM) versus...
T5197 BIBF0775 BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).
T5125 LY3200882 LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
T1977 Dorsomorphin Dorsomorphin is an effective and specific inhibitor of AMPK (AMP-activated protein kinase), which is induced by AICAR and metformin.
T2896 Alantolactone Alantolactone(Alant camphor), a sesquiterpene lactone, has potential activity against triple-negative breast Y MDA-MB-231 cells by suppressing the signal transdu...
T2098 A 77-01 A 77-01 is a potent inhibitor of TGF-(beta) type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.
T2803 Monocrotaline Monocrotaline is a pyrrolizidine alkaloid and a toxic plant constituent that poisons livestock and humans through the ingestion of contaminated grains and other ...
T5129 SRI-011381 hydrochloride SRI-011381, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.
T3924 Astragaloside II Astragaloside II is an effective MDR reversal agent and may be a potential adjunctive agent for hepatic cancer chemotherapy. Astragaloside II also induces osteog...
T1943 ML347 ML347(DN193719) is a highly specific ALK1/2 inhibitor ( IC50: 46/32 nM), and the selectivity for ALK2 is >300-fold than ALK3.
T3025 Asiaticoside Asiaticoside (Madecassol) is the active chemical component of the plant Centella asiatica. Asiaticoside is used to study potential treatments for wounds and burn...
T16708 R-268712 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 ...
T6496 Vactosertib Vactosertib is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as act...
TN1040 Skullcapflavone II Skullcapflavone II is a flavonoid derived from Scutellaria baicalensis, a widely used herbal medicine in anti-inflammatory and anticancer therapy. Skullcapflavon...
T4975 SM 16 SM 16 is a ALK5/ALK4 kinase inhibitor (Ki: 10/1.5 nM).
T1914 K02288 K02288 is a novel small molecule inhibitor of ALK1/2/3/6.
T8785 HALOFUGINONE LACTATE HALOFUGINONE LACTATE is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.Halofuginone ...
T2123 LY2109761 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 phosph...
T2754 Oxymatrine Oxymatrine is an alkaloid isolated from Sophora flavescens, used as the antibiotic. It is a traditional Chinese medicine used in the treatment against hepatitis ...
T1944 LDN-214117 LDN-214117 is a potent and selective ALK2 inhibitor.
T2416 BIX02189 BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
T1763 SB 525334 SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM).
T1726 SB-431542 SB-431542 is a potent and selective inhibitor of ALK5 (IC50: 94 nM) and is also an inhibitor of ALK4 (IC50: 140 nM) and ALK7.
SIS3 free base
T12923
SIS3 free base is a potent and selective Smad3 phosphorylation inhibitor. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
LSKL, Inhibitor of Thrombospondin (TSP-1)
T7377
LSKL, Inhibitor of Thrombospondin (TSP-1) is a peptide derived from the latency-associated peptide, inhibits thrombospondin (TSP-1) activation of TGF-β.
LDN-193189 2HCl
T35348
Dalbergioidin
TN3753
Dalbergioidin exhibits tyrosinase inhibitory activity with an IC50 of 20 mM. It shows a melanin biosynthesis inhibition zone in the culture plate of Streptomyces...
TGFβRI-IN-1
T13137
TGFβRI-IN-1 is an oral active and selective inhibitor of TGFβ receptor type I (TGFβRI) kinase(IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respec...
Chromenone 1
T61301
Chromenone 1 is a potent potentiator of osteogenic bone morphogenetic protein (BMP). Chromenone 1 induces a pronounced, kinase-independent, negative TGFβ feedba...
Pentabromophenol
T20319
Pentabromophenol inhibits TGF-β signaling by accelerating the degradation of type II TGF-β receptors via caveolae-mediated endocytosis.
TP0427736
T24897
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...
TGFβRI-IN-3
T9523
TGFβRI-IN-3 inhibits TGFβR1 with an IC 50 of 0.79 nM with 2000-fold selectivity against MAP4K4. TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor that has p...
PF-06952229
T12433
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.
LSKL, Inhibitor of Thrombospondin TSP-1 acetate
T7676
LSKL, Inhibitor of Thrombospondin TSP-1 acetate is activation of TGF-β .
Disitertide acetate
T11052L
Disitertide acetate is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disiter...
Kartogenin
T1748
Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.
Halofuginone hydrobromide
T3524
Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of...
Halofuginone
T6856
Halofuginone, 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...
A 83-01
T3031
A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 with IC50 values of 12 ...
SD-208
T2109
SD-208, a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII.
GW788388
T1800
GW788388 is a potent and selective inhibitor of ALK5, also inhibits TGF-(beta) type II receptor and activin type II receptor activities.
BMS986260
T8730
BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
Hesperetin
T2565
Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges....
RepSox
T6337
RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor.
(E)-SIS3
T3636
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 signal...
Chebulinic acid
TQ0184
Chebulinic acid is a potent inhibitor of M. tuberculosis DNA gyrase. It also can inhibit SMAD-3 phosphorylation and H+ K+-ATPase activity.
LDN193189
T1935
LDN193189 (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)....
SRI-011381
T4283
SRI-011381, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.
BIX02188
T6324
BIX02188 is a specific MEK5 inhibitor (IC50: 4.3 nM), also inhibits ERK5 catalytic activity (IC50: 810 nM), and does not inhibit closely related kinases MEK1/2, ...
SJ000291942
T4662
SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway.
LDN-212854
T1900
LDN-212854, a novel BMP inhibitor, exhibits greater selectivity for BMP versus the TGF-β type I receptors; possesses differences towards ALK2(IC50=1.3 nM) versu...
BIBF0775
T5197
BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).
LY3200882
T5125
LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
Dorsomorphin
T1977
Dorsomorphin is an effective and specific inhibitor of AMPK (AMP-activated protein kinase), which is induced by AICAR and metformin.
Alantolactone
T2896
Alantolactone(Alant camphor), a sesquiterpene lactone, has potential activity against triple-negative breast Y MDA-MB-231 cells by suppressing the signal transdu...
A 77-01
T2098
A 77-01 is a potent inhibitor of TGF-(beta) type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.
Monocrotaline
T2803
Monocrotaline is a pyrrolizidine alkaloid and a toxic plant constituent that poisons livestock and humans through the ingestion of contaminated grains and other ...
SRI-011381 hydrochloride
T5129
SRI-011381, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.
Astragaloside II
T3924
Astragaloside II is an effective MDR reversal agent and may be a potential adjunctive agent for hepatic cancer chemotherapy. Astragaloside II also induces osteog...
ML347
T1943
ML347(DN193719) is a highly specific ALK1/2 inhibitor ( IC50: 46/32 nM), and the selectivity for ALK2 is >300-fold than ALK3.
Asiaticoside
T3025
Asiaticoside (Madecassol) is the active chemical component of the plant Centella asiatica. Asiaticoside is used to study potential treatments for wounds and burn...
R-268712
T16708
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...
Vactosertib
T6496
Vactosertib is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as act...
Skullcapflavone II
TN1040
Skullcapflavone II is a flavonoid derived from Scutellaria baicalensis, a widely used herbal medicine in anti-inflammatory and anticancer therapy. Skullcapflavon...
SM 16
T4975
SM 16 is a ALK5/ALK4 kinase inhibitor (Ki: 10/1.5 nM).
K02288
T1914
K02288 is a novel small molecule inhibitor of ALK1/2/3/6.
HALOFUGINONE LACTATE
T8785
HALOFUGINONE LACTATE is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.Halofuginone ...
LY2109761
T2123
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 phos...
Oxymatrine
T2754
Oxymatrine is an alkaloid isolated from Sophora flavescens, used as the antibiotic. It is a traditional Chinese medicine used in the treatment against hepatitis ...
LDN-214117
T1944
LDN-214117 is a potent and selective ALK2 inhibitor.
BIX02189
T2416
BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
SB 525334
T1763
SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM).
SB-431542
T1726
SB-431542 is a potent and selective inhibitor of ALK5 (IC50: 94 nM) and is also an inhibitor of ALK4 (IC50: 140 nM) and ALK7.
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