TGF-β / Smad Inhibitors

Inhibitory Selectivity
Catalog No.Inhibitor Name ALK1ALK2ALK3ALK4TGFβRI/ALK5ALK6ALK7TGFβRIITGF-βSmad3Other
A10826SB431542
**
A11205LDN-193189
****
***
A11017Galunisertib
**
A11133LY2109761
***
*
A10827SB525334
***
A11157SB505124
**
**
A11083GW788388
***
A13446LY364947
**
*
RIPK2,CK1δ,MLK-7K
A11762RepSox
****
A11478LDN-193189 HCl
****
***
A14311K02288
****
****
***
*
*
****
A16096LDN-214117
***
A14066SD-208
**
A14213EW-7197
***
****
A14298ML347
**
***
*
*
A12821LDN-212854
****
****
**
*
*
A12820DMH1
**
A16209Pirfenidone
A10449Hesperetin
Histamine receptor
A12358A 83-01
***
**
****
A12924ITD 1
*
A14436A 77-01
***
A16065SIS3
A16207R-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.



31 Item(s)

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Catalog No. Product Name Application Product Information
A11017 SALE

LY2157299

TGF-βR Inhibitor
LY2157299 is an orally active transforming growth factor beta receptor (TGF-βR) kinase inhibitor.
A14311 SALE

K02288

BMP inhibitor
K02288 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.
A14436

A 77-01

ALK5 inhibitor
A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.
A13446 SALE

LY364947

TGFβR-I Inhibitor
LY364947 is a diheteroaryl-substituted pyrazole compound used as a selective, ATP-competitive inhibitor of TGF-βRI (TGF-β Receptor I kinase).
A14810

Alantolactone

-
Alantolactone, an allergenic sesquiterpene lactone, has recently been found to have significant antitumor effects on malignant tumor cells.
A15185

NG25

TAK1/MAP4K2 inhibitor
NG25, 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.
A15232

SB-505124 HCl

TGF-β Receptors Inhibitor
SB-505124 hydrochloride is an inhibitor of activin receptor-like kinases (ALKs).
A14066

SD-208

TGF-βR Inhibitor
SD-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.
A16065 SALE

SIS3

Smad3 inhibitor
SIS3 is a novel specific inhibitor of Smad3. It has effect on transforming growth factor-beta1-induced extracellular matrix expression.
A16073

(+)-ITD 1

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.
A16096

LDN-214117

ALK2 inhibitor
LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM.
A16207

R-268712

ALK5 inhibitor
R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
A16208

Chebulinic acid

-
Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
A16209

Pirfenidone

-
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.
A14298 SALE

ML347

BMP receptor inhibitor
ML347 is a selective BMP receptor inhibitor .
A11478 SALE

LDN193189 HCl

-
LDN193189 HCl is the hydrochloride salt of LDN193189.
A14213 SALE

EW-7197

ALK4/ALK5 inhibitor
EW-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
A10826 SALE

SB 431542

TGF-beta/Smad inhibitor
SB 431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7 .
A11083 SALE

GW788388

TGF-beta/Smad inhibitor
GW788388 is a potent, orally active and selective inhibitor of transforming growth factor beta receptor I (TGF-βR1) (activin receptor-like kinase 5, ALK5).
A11157 SALE

SB-505124

ALK5 inhibitor
SB-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).
A11205 SALE

LDN193189

ALK inhibitor
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.
A10827 SALE

SB 525334

ALK Inhibitor
SB525334 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
A11133 SALE

LY2109761

TβRI/II kinase inhibitor
LY2109761, a novel transforming growth factor β receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis
A10449 SALE

Hesperetin

PDE4 inhibitor
Hesperetin, 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.
A11762 SALE

RepSox (SJN 2511)

-
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).
A12358 SALE

A 83-01

TGF-β/ALK5 inhibitor
A83-01 is a TGF-β kinase/activin receptor like kinase (ALK5) inhibitor.
A12820 SALE

DMH-1

ALK2 inhibitor
DMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM).
A12821 SALE

LDN-212854

BMP receptor inhibitor
LDN-212854 is an ALK2-Biased BMP Type I Receptor Kinase Inhibitor.
A12924 SALE

ITD-1

TGF-β inhibitor
ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells.
A12926 SALE

Kartogenin

Smad inhibitor
Kartogenin potently induces differentiation of human mesenchymal stem cells into chondrocytes
A16210

SRI-011381 hydrochloride

TGF-beta agonist
SRI-011381 hydrochloride is a TGF-beta signaling agonist.

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