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.
Inhibitors Catalog Download
产品编号 产品名称
T2510 GalunisertibHOT Galunisertib is an orally available inhibitor of TGFβRI kinase (IC50: 56 nM) with potential antineoplastic activity.
T2123 LY2109761HOT 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...
T1763 SB 525334HOT SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM).
T9523 TGFβRI-IN-3 TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor with potential application in immuno-oncology.
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....
T3674 Hydroxysafflor yellow A Hydroxysafflor yellow A inhibited adipogenesis by increasing HSL promoter activities. Hydroxysafflor yellow A can effectively protect the liver from long-term al...
T2109 SD-208 SD-208, a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII.
T2386 Pirfenidone Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production. Pirfenidone inhibits fibroblast, epidermal, platelet-derived, and tr...
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 signal...
T1748 Kartogenin Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.
T4283 SRI-011381 SRI-011381, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.
T6337 RepSox RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor.
T2048 LY-364947 LY364947 is a potent ATP-competitive inhibitor of TGFβR-I.
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 ...
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...
T2273 ITD-1 ITD-1 is a potent and highly selective TGFβ pathway inhibitor.
T2416 BIX02189 BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
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...
T4662 SJ000291942 SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ)...
T24897 TP0427736 TP0427736 is a potent and selective inhibitor of ALK5 with an IC50 of 2.72 nM, 300-fold higher than the inhibitory effect on ALK3. TP0427736 reduces TGF-β-induc...
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.
T20319 Pentabromophenol Pentabromophenol suppressed TGF-β response by accelerating the turnover rate of TGF-β receptors.
T8785 HALOFUGINONE LACTATE HALOFUGINONE LACTATE is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.Halofuginone ...
T8730 BMS986260 BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
T8730 BMS986260 BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
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, respec...
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...
T5125 LY3200882 LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
TN1040 Skullcapflavone II Skullcapflavone II is a flavonoid derived from Scutellaria baicalensis, a widely used herbal medicine in anti-inflammatory and anticancer therapy. Skullcapflavo...
T8330 BIO-013077-01 BIO-013077-01 is a potent TGFbeta family type I receptors antagonist.
T7799 BMP signaling agonist sb4 SB 4 is an agonist of benzoxazole bone morphogenetic protein (BMP) signaling (EC50 :74 nM)
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.
T7676 LSKL, Inhibitor of Thrombospondin TSP-1 LSKL, Inhibitor of Thrombospondin TSP-1(TSP-1) is activation of TGF-β .
T5197 BIBF0775 BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).
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.
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, ...
Galunisertib HOT
T2510CAS 700874-72-2
Galunisertib is an orally available inhibitor of TGFβRI kinase (IC50: 56 nM) with potential antineoplastic activity.
LY2109761 HOT
T2123CAS 700874-71-1
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 phos...
SB 525334 HOT
T1763CAS 356559-20-1
SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM).
TGFβRI-IN-3
T9523CAS T9523
TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor with potential application in immuno-oncology.
Hesperetin
T2565CAS 520-33-2
Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges....
Hydroxysafflor yellow A
T3674CAS 78281-02-4
Hydroxysafflor yellow A inhibited adipogenesis by increasing HSL promoter activities. Hydroxysafflor yellow A can effectively protect the liver from long-term al...
SD-208
T2109CAS 627536-09-8
SD-208, a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII.
Pirfenidone
T2386CAS 53179-13-8
Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production. Pirfenidone inhibits fibroblast, epidermal, platelet-derived, and tr...
(E)-SIS3
T3636CAS 521984-48-5
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...
Kartogenin
T1748CAS 4727-31-5
Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.
SRI-011381
T4283CAS 1629138-41-5
SRI-011381, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.
RepSox
T6337CAS 446859-33-2
RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor.
LY-364947
T2048CAS 396129-53-6
LY364947 is a potent ATP-competitive inhibitor of TGFβR-I.
Monocrotaline
T2803CAS 315-22-0
Monocrotaline is a pyrrolizidine alkaloid and a toxic plant constituent that poisons livestock and humans through the ingestion of contaminated grains and other ...
Asiaticoside
T3025CAS 16830-15-2
Asiaticoside (Madecassol) is the active chemical component of the plant Centella asiatica. Asiaticoside is used to study potential treatments for wounds and burn...
ITD-1
T2273CAS 1099644-42-4
ITD-1 is a potent and highly selective TGFβ pathway inhibitor.
BIX02189
T2416CAS 1094614-85-3
BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM.
Astragaloside II
T3924CAS 84676-89-1
Astragaloside II is an effective MDR reversal agent and may be a potential adjunctive agent for hepatic cancer chemotherapy. Astragaloside II also induces osteog...
SJ000291942
T4662CAS 425613-09-8
SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ)...
TP0427736
T24897CAS 864374-00-5
TP0427736 is a potent and selective inhibitor of ALK5 with an IC50 of 2.72 nM, 300-fold higher than the inhibitory effect on ALK3. TP0427736 reduces TGF-β-induc...
SIS3 free base
T12923CAS 1009104-85-1
SIS3 free base is a potent and selective Smad3 phosphorylation inhibitor. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
Pentabromophenol
T20319CAS 608-71-9
Pentabromophenol suppressed TGF-β response by accelerating the turnover rate of TGF-β receptors.
HALOFUGINONE LACTATE
T8785CAS 82186-71-8
HALOFUGINONE LACTATE is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.Halofuginone ...
BMS986260
T8730CAS 2001559-19-7
BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
BMS986260
T8730CAS 2001559-19-7
BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
Dalbergioidin
TN3753CAS 30368-42-4
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
T13137CAS 1950628-94-0
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...
Rubrofusarin gentiobioside
TN2165CAS 24577-90-0
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...
LY3200882
T5125CAS 1898283-02-7
LY3200882 is a highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
Skullcapflavone II
TN1040CAS 55084-08-7
Skullcapflavone II is a flavonoid derived from Scutellaria baicalensis, a widely used herbal medicine in anti-inflammatory and anticancer therapy. Skullcapflavo...
BIO-013077-01
T8330CAS 746667-48-1
BIO-013077-01 is a potent TGFbeta family type I receptors antagonist.
BMP signaling agonist sb4
T7799CAS 100874-08-6
SB 4 is an agonist of benzoxazole bone morphogenetic protein (BMP) signaling (EC50 :74 nM)
Chebulinic acid
TQ0184CAS 18942-26-2
Chebulinic acid is a potent inhibitor of M. tuberculosis DNA gyrase. It also can inhibit SMAD-3 phosphorylation and H+ K+-ATPase activity.
LSKL, Inhibitor of Thrombospondin TSP-1
T7676CAS T7676
LSKL, Inhibitor of Thrombospondin TSP-1(TSP-1) is activation of TGF-β .
BIBF0775
T5197CAS 334951-90-5
BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).
SRI-011381 hydrochloride
T5129CAS 2070014-88-7
SRI-011381, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.
BIX02188
T6324CAS 1094614-84-2
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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