TGF-β / Smad Inhibitors
Catalog No. | Inhibitor Name | ALK1 | ALK2 | ALK3 | ALK4 | TGFβRI/ALK5 | ALK6 | ALK7 | TGFβRII | TGF-β | Smad3 | Other |
---|---|---|---|---|---|---|---|---|---|---|---|---|
A10826 | SB431542 | ** | ||||||||||
A11205 | LDN-193189 | **** | *** | |||||||||
A11017 | Galunisertib | ** | ||||||||||
A11133 | LY2109761 | *** | * | |||||||||
A10827 | SB525334 | *** | ||||||||||
A11157 | SB505124 | ** | ** | |||||||||
A11083 | GW788388 | *** | ||||||||||
A13446 | LY364947 | ** | * | RIPK2,CK1δ,MLK-7K | ||||||||
A11762 | RepSox | **** | ||||||||||
A11478 | LDN-193189 HCl | **** | *** | |||||||||
A14311 | K02288 | **** | **** | *** | * | * | **** | |||||
A16096 | LDN-214117 | *** | ||||||||||
A14066 | SD-208 | ** | ||||||||||
A14213 | EW-7197 | *** | **** | |||||||||
A14298 | ML347 | ** | *** | * | * | |||||||
A12821 | LDN-212854 | **** | **** | ** | * | * | ||||||
A12820 | DMH1 | ** | ||||||||||
A16209 | Pirfenidone | |||||||||||
A10449 | Hesperetin | Histamine receptor | ||||||||||
A12358 | A 83-01 | *** | ** | **** | ||||||||
A12924 | ITD 1 | * | ||||||||||
A14436 | A 77-01 | *** | ||||||||||
A16065 | SIS3 | |||||||||||
A16207 | R-268712 | **** |
Notes:
1.Hover mouse over " " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
-
SB 431542
Catalog No. A10826 TGF-beta/Smad inhibitorSB 431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I ALK receptors ALK4, ALK5, and ALK7 . Learn More -
LY2157299
Catalog No. A11017 TGF-βR InhibitorLY2157299 is an orally active transforming growth factor beta receptor (TGF-βR) kinase inhibitor. Learn More -
LDN193189
Catalog No. A11205 ALK inhibitorLDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation. Learn More -
LY2109761
Catalog No. A11133 TβRI/II kinase inhibitorLY2109761, a novel transforming growth factor β receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis Learn More -
RepSox (SJN 2511)
Catalog No. A11762 RepSox (SJN 2511) is a selective inhibitor of the TGF-β type I receptor ALK5 (IC50 values are 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding respectively). Learn More -
SIS3
Catalog No. A16065 Smad3 inhibitorSIS3 is a novel specific inhibitor of Smad3. It has effect on transforming growth factor-beta1-induced extracellular matrix expression. Learn More -
DMH-1
Catalog No. A12820 ALK2 inhibitorDMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM). Learn More -
ITD-1
Catalog No. A12924 TGF-β inhibitorITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells. Learn More -
LDN193189 HCl
Catalog No. A11478 LDN193189 HCl is the hydrochloride salt of LDN193189. LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation. Learn More -
EW-7197 (Vactosertib)
Catalog No. A14213 ALK4/ALK5 inhibitorEW-7197 is a highly potent, selective, and orally bioavailable TGF-β I receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively Learn More -
NG25
Catalog No. A15185 TAK1/MAP4K2 inhibitorNG25, a TAK1 inhibitor, inhibited the activation of IKK by TLR7 and TLR9 agonists and prevented the secretion of type 1 IFNs induced by these ligands in Gen2.2 cells. Learn More -
TGFβRI-IN-1
Catalog No. A18800 TGFβRI kinase inhibitorTGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively. Learn More -
SB-505124 HCl
Catalog No. A15232 -
SD-208
Catalog No. A14066 TGF-βR InhibitorSD-208 is a potent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50= 49 nM); displays > 100-fold and > 17-fold selectivity over TGF-βRII and other common kinases respectively. Learn More -
(+)-ITD 1
Catalog No. A16073 TGF-β inhibitor(+)-ITD-1 is a resolved enantiomer of ITD-1 that possesses a greater than 2-fold increase in TGF-β inhibition (~400 nM) and 1.3-fold increase in cardiogenesis compared to the racemic ITD-1. Learn More -
LDN-214117
Catalog No. A16096 ALK2 inhibitorLDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM. Learn More -
R-268712
Catalog No. A16207 ALK5 inhibitorR-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM. Learn More -
Chebulinic acid
Catalog No. A16208 Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity. Learn More -
Pirfenidone
Catalog No. A16209 Pirfenidone is an anti-fibrotic drug for the treatment of idiopathic pulmonary fibrosis (IPF). It works by reducing lung fibrosis through downregulation of the production of growth factors and procollagens I and II. Learn More -
SRI-011381 hydrochloride
Catalog No. A16210 -
LY 3200882
Catalog No. A16816 TGFβRI inhibitorLY 3200882 is a potent, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). It potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion. Learn More -
-
New
BIBF0775
Catalog No. A17230 TGFβRI inhibitorBIBF0775 is an inhibitor of the transforming growth factor β receptor I (TGFβRI). Learn More -
-
Alantolactone
Catalog No. A14810 Alantolactone, an allergenic sesquiterpene lactone, has recently been found to have significant antitumor effects on malignant tumor cells. Learn More -
LY364947
Catalog No. A13446 TGFβR-I InhibitorLY364947 is a diheteroaryl-substituted pyrazole compound used as a selective, ATP-competitive inhibitor of TGF-βRI (TGF-β Receptor I kinase). Learn More -
A 77-01
Catalog No. A14436 ALK5 inhibitorA 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM. Learn More -
K02288
Catalog No. A14311 BMP inhibitorK02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6. Learn More -
ML347
Catalog No. A14298 BMP receptor inhibitorML347 is a selective BMP receptor inhibitor . Learn More -
Kartogenin
Catalog No. A12926 Smad inhibitorKartogenin potently induces differentiation of human mesenchymal stem cells into chondrocytes Learn More -
LDN-212854
Catalog No. A12821 BMP receptor inhibitorLDN-212854 is an ALK2-Biased BMP Type I Receptor Kinase Inhibitor. Learn More -
A 83-01
Catalog No. A12358 TGF-β/ALK5 inhibitorA83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor ALK7 Learn More -
Hesperetin
Catalog No. A10449 PDE4 inhibitorHesperetin, a selective phosphodiesterase (PDE)4 inhibitor, is present in the traditional Chinese medicine, “Chen Pi.” Hesperetin is a citrus flavonoid that has been reported to lower plasma cholesterol. Hesperetin reduces the transcription of ACAT-2 mRNA in Hep-G2 cells and reduces ApoB protein synthesis in a dose-dependent manner. It also is a potential therapy for carcinoid cancer. Learn More -
SB 525334
Catalog No. A10827 ALK InhibitorSB525334 is a selective inhibitor of transforming growth factor-β receptor I (ALK5, TGF-βRI) (IC50 = 14.3 nM). Inhibits TGF-β1-induced smad2/3 nuclear localization and TGF-βRI-induced mRNA expression in kidney cells Learn More -
SB-505124
Catalog No. A11157 ALK5 inhibitorSB-505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5), ALK4 and ALK7 (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively). Learn More -
GW788388
Catalog No. A11083 TGF-beta/Smad inhibitorGW788388 is a potent, orally active and selective inhibitor of transforming growth factor beta receptor I (TGF-βR1) (activin receptor-like kinase 5, ALK5). Learn More