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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.
Cat No. product name
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...
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...
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 ...
T9523 TGFβRI-IN-3 TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor with potential application in immuno-oncology.
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...
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...
T1800 GW788388 GW788388 is a potent and selective inhibitor of ALK5, also inhibits TGF-(beta) type II receptor and activin type II receptor activities.
T1914 K02288 K02288 is a novel small molecule inhibitor of ALK1/2/3/6.
T2462 SB-505124 SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5.
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...
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.
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...
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...
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.
T20319 Pentabromophenol Pentabromophenol inhibits TGF-β signaling by accelerating the degradation of type II TGF-β receptors via caveolae-mediated endocytosis.
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 ...
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)....
T4975 SM 16 SM 16 is a ALK5/ALK4 kinase inhibitor (Ki: 10/1.5 nM).
TN1040 Skullcapflavone II Skullcapflavone II is a flavonoid derived from Scutellaria baicalensis, a widely used herbal medicine in anti-inflammatory and anticancer therapy. Skullcapflavon...
T2048 LY-364947 LY364947 is a potent ATP-competitive inhibitor of TGFβR-I.
T1977 Dorsomorphin Dorsomorphin is an effective and specific inhibitor of AMPK (AMP-activated protein kinase), which is induced by AICAR and metformin.
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...
T1942 DMH-1 DMH-1 is a potent and selective BMP inhibitor.
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....
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.
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...
T2386 Pirfenidone Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production. Pirfenidone inhibits fibroblast, epidermal, platelet-derived, and tran...
T6146 Dorsomorphin dihydrochloride Dorsomorphin is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.
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.
T1944 LDN-214117 LDN-214117 is a potent and selective ALK2 inhibitor.
T35348 LDN-193189 2HCl LDN-193189 (DM3189) 2HCl是一种选择性 BMP 信号抑制剂,抑制ALK1,ALK2,ALK3和ALK6,在激酶测定中的 IC50 分别为 0.8 nM、0.8 nM、5.3 nM 和 16.7 nM。LDN-193189 抑制BMP I型受体ALK2和ALK3的转录活性,在C2C12细胞中IC50分...
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.
T2109 SD-208 SD-208, a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII.
T2273 ITD-1 ITD-1 is a potent and highly selective TGFβ pathway inhibitor.
T2510 Galunisertib Galunisertib is an orally available inhibitor of TGFβRI kinase (IC50: 56 nM) with potential antineoplastic activity.
T2416 BIX02189 BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 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 ...
TN2165 Rubrofusarin gentiobioside Rubrofusarin-6-O-beta-D-gentiobioside can significantly decrease the expression of TGF-beta1 and fibronectin and NF-kappaB DNA binding activity, suggests that it...
T8730 BMS986260 BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
T8785 HALOFUGINONE LACTATE HALOFUGINONE LACTATE is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.Halofuginone ...
T8330 BIO-013077-01 BIO-013077-01 is a potent TGFbeta family type I receptors antagonist.
T7676 LSKL, Inhibitor of Thrombospondin TSP-1 acetate LSKL, Inhibitor of Thrombospondin TSP-1 acetate is activation of TGF-β .
T7799 BMP signaling agonist sb4 SB 4 is an agonist of benzoxazole bone morphogenetic protein (BMP) signaling (EC50 :74 nM)
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.
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...
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...
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.
T5125 LY3200882 LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
T5197 BIBF0775 BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).
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, ...
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...
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...
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 ...
TGFβRI-IN-3
T9523
TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor with potential application in immuno-oncology.
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...
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...
GW788388
T1800
GW788388 is a potent and selective inhibitor of ALK5, also inhibits TGF-(beta) type II receptor and activin type II receptor activities.
K02288
T1914
K02288 is a novel small molecule inhibitor of ALK1/2/3/6.
SB-505124
T2462
SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5.
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...
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.
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...
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...
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.
Pentabromophenol
T20319
Pentabromophenol inhibits TGF-β signaling by accelerating the degradation of type II TGF-β receptors via caveolae-mediated endocytosis.
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...
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)....
SM 16
T4975
SM 16 is a ALK5/ALK4 kinase inhibitor (Ki: 10/1.5 nM).
Skullcapflavone II
TN1040
Skullcapflavone II is a flavonoid derived from Scutellaria baicalensis, a widely used herbal medicine in anti-inflammatory and anticancer therapy. Skullcapflavon...
LY-364947
T2048
LY364947 is a potent ATP-competitive inhibitor of TGFβR-I.
Dorsomorphin
T1977
Dorsomorphin is an effective and specific inhibitor of AMPK (AMP-activated protein kinase), which is induced by AICAR and metformin.
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...
DMH-1
T1942
DMH-1 is a potent and selective BMP inhibitor.
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....
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.
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 ...
Pirfenidone
T2386
Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production. Pirfenidone inhibits fibroblast, epidermal, platelet-derived, and tr...
Dorsomorphin dihydrochloride
T6146
Dorsomorphin is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.
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.
LDN-214117
T1944
LDN-214117 is a potent and selective ALK2 inhibitor.
LDN-193189 2HCl
T35348
LDN-193189 (DM3189) 2HCl是一种选择性 BMP 信号抑制剂,抑制ALK1,ALK2,ALK3和ALK6,在激酶测定中的 IC50 分别为 0.8 nM、0.8 nM、5.3 nM 和 ...
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.
SD-208
T2109
SD-208, a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII.
ITD-1
T2273
ITD-1 is a potent and highly selective TGFβ pathway inhibitor.
Galunisertib
T2510
Galunisertib is an orally available inhibitor of TGFβRI kinase (IC50: 56 nM) with potential antineoplastic activity.
BIX02189
T2416
BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 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 ...
Rubrofusarin gentiobioside
TN2165
Rubrofusarin-6-O-beta-D-gentiobioside can significantly decrease the expression of TGF-beta1 and fibronectin and NF-kappaB DNA binding activity, suggests that it...
BMS986260
T8730
BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
HALOFUGINONE LACTATE
T8785
HALOFUGINONE LACTATE is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.Halofuginone ...
BIO-013077-01
T8330
BIO-013077-01 is a potent TGFbeta family type I receptors antagonist.
LSKL, Inhibitor of Thrombospondin TSP-1 acetate
T7676
LSKL, Inhibitor of Thrombospondin TSP-1 acetate is activation of TGF-β .
BMP signaling agonist sb4
T7799
SB 4 is an agonist of benzoxazole bone morphogenetic protein (BMP) signaling (EC50 :74 nM)
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.
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...
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...
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.
LY3200882
T5125
LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
BIBF0775
T5197
BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).
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, ...
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