|
T3636 |
(E)-SIS3
|
SIS3,SIS3 HCl |
TGF-beta/Smad
|
|
(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 signaling. It also inhibits TGF-β1-induced myofibroblas... |
|
T0459 |
Sulindac
|
Arthrocine,MK-231,Clinoril,Sulindac sulfoxide |
COX
,
Autophagy
|
|
Sulindac (Sulindac sulfoxide) is a sulfinylindene derivative prodrug with potential antineoplastic activity. Converted in vivo to an active metabolite, sulindac, a nonsteroidal anti-inflammatory drug (NSAID), blocks cycl... |
|
T61389 |
TGFβ1-IN-1
|
|
TGF-beta/Smad
|
|
TGFβ1-IN-1 is an orally active TGF-β1 inhibitor that inhibits the production of TGF-β1-induced fibrotic markers (α-SMA and fibronectin) and can be used for the study of cancer and autoimmune diseases. |
|
T73300 |
AXL-IN-13
|
|
FLT
,
TAM Receptor
,
PDGFR
,
TGF-beta/Smad
|
|
AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 value of 1.6 nM and a Kd value of 0.26 nM.AXL-IN-13 exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) and inh... |
|
T1763 |
SB 525334
|
SB525334 |
ALK
,
TGF-beta/Smad
|
|
SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM). |
|
T38752 |
EW-7195
|
|
ALK
,
TGF-beta/Smad
|
|
EW-7195 is a selective and potent inhibitor of ALK5 (TGFβR1) with an IC50 value of 4.83 nM.EW-7195 has an affinity for ALK5 that is more than 300-fold higher than that of p38α.EW-7195 has an inhibitory effect on TGF-β1-i... |
|
T32613 |
LCB 03-0110 dihydrochloride
|
|
Src
|
|
LCB 03-0110 Dihydrochloride is a potent inhibitor of the c-Src kinase (IC50 = 1.3 nM) and tyrosine kinases in the BTK and SYK family, as well as in the DDR2 family. It inhibits LPS-induced activation of macrophages and T... |
|
T11052L |
Disitertide acetate
|
P144 acetate,Disitertide acetate(272105-42-7 Free base) |
TGF-beta/Smad
|
|
Disitertide acetate (P144 acetate) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide acetate is also a PI3K inhibitor and an ... |
|
T9953 |
BT173
|
|
Others
|
|
BT173 is a novel inhibitor of homeodomain interacting protein kinase 2 (HIPK2 ), attenuating renal fibrosis through suppression of the TGF-ß1/Smad3 pathway. |
|
T11793 |
KY-05009
|
|
Wnt/beta-catenin
|
|
KY-05009 is a chemical compound that effectively suppresses TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells, reduces TNIK protein expression and the transcriptional activity o... |
|
T62483 |
CJJ300
|
|
TGF-beta/Smad
|
|
CJJ300 is a transforming growth factor-β (TGF-β) inhibitor (IC50 : 5.3 μM).CJJ300 inhibits TGF-β signaling by disrupting the formation of the TGF-β-TβR-I-TβR-II signaling complex.CJJ300 inhibits cell migration. |
|
T76066 |
Pm26TGF-β1 peptide
|
|
|
|
pm26TGF-β1 peptide, mimicking a portion of the human TGF-β1 molecule, demonstrates a high affinity for the TGF-β1 receptor. It exhibits potent anti-inflammatory properties without inducing neutrophils' chemoattraction [1... |
|
T76066L |
Pm26TGF-β1 peptide TFA
|
|
|
|
pm26TGF-β1 TFA peptide is a synthetic peptide that emulates a segment of the human TGF-β1 molecule, demonstrating high affinity for the TGF-β1 receptor. It possesses potent anti-inflammatory capabilities while lacking th... |
|
T80272 |
Vicatertide
|
SB-01 |
|
|
Vicatertide is an inhibitor of transforming growth factor beta-1 (TGF-β1) [1]. |
|
T69517 |
Bexotegrast HCl
|
|
|
|
Bexotegrast, also known as PLN-74809, is a small-molecule, dual selective inhibitor of αVβ1 / αVβ6 for idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). These integrins cause upstream activati... |
|
T24470 |
Mitochonic Acid 35
|
MA35,MA-35,MA 35,Mitochonic Acid-35 |
|
|
Mitochonic Acid 35 is a dual TNF-α and TGF-β1 inhibitor that acts by inhibiting IκB kinase phosphorylation and Smad3 phosphorylation. |
|
T12923 |
(Rac)-SIS3 free base
|
|
TGF-beta/Smad
|
|
SIS3 free base is a potent and selective Smad3 phosphorylation inhibitor. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1. |
|
T76498 |
H-Leu-Ser-Lys-Leu-OH
|
|
|
|
H-Leu-Ser-Lys-Leu-OH (LSYL), a latency-associated peptide located at the amino terminus of LAP, exhibits an inhibitory effect on TGF-β1 activation. By binding with KRFK, it obstructs TGF-β1 signal transduction, thereby i... |
|
T11052 |
Disitertide
|
P144 |
Others
|
|
Disitertide (P144) is an inhibitor of TGF-β1. |
|
TP2147 |
LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
|
|
Others
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA, a latency-associated protein (LAP)-TGFβ derived tetrapeptide, is a competitive antagonist of TGF-β1. |
|
T77189 |
Sudubrilimab
|
|
|
|
Sudubrilimab (HS636), an Ig G1-kappa monoclonal antibody targeting PDL1, is engineered with a TGF-β1 receptor II ectodomain (TGFBR2-ECD) fused to its C-terminus. This design enables Sudubrilimab to simultaneously inhibit... |
|
T79789 |
DT-6
|
|
TGF-beta/Smad
|
|
DT-6, a potent TGF-β1 inhibitor, impedes M2 macrophage-induced epithelial-to-mesenchymal transition and the invasive migration of cancer cells, thereby showing potential for cancer research applications [1]. |
|
T3689L |
Ruboxistaurin mesylate
|
LY-333531,LY333531,LY 333531,LY-333531 Mesylate |
|
|
Ruboxistaurin is a PKC beta inhibitor. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin attenuates diabetic ne... |
|
T78944 |
VDR agonist 2
|
|
|
|
VDR agonist 2 (compound 16i), a vitamin D receptor (VDR) agonist, effectively inhibits TGF-β1-induced hepatic stellate cell (HSC) activation, demonstrating notable anti-hepatic fibrosis efficacy both in vitro and in vivo... |
|
T74432 |
Mongersen
|
|
|
|
Mongersen (GED-0301), a specific and orally active SMAD7 antisense oligonucleotide, enhances TGF-β1 activity, reducing inflammatory signals. It has been shown to alleviate experimental colitis resembling Crohn's disease ... |
|
T79603 |
3,7-DMF
|
|
TGF-beta/Smad
|
|
3,7-Dimethylfumarate (3,7-DMF) serves as an oral inhibitor of transforming growth factor-beta 1 (TGF-β1)-mediated hepatic stellate cell (HSC) activation. By inducing antioxidant gene expression and scavenging reactive ox... |
|
T73035 |
STAT3-IN-15
|
|
|
|
STAT3-IN-15, a potent and orally active inhibitor targeting STAT3, effectively combats idiopathic pulmonary fibrosis (IPF) by hindering STAT3 phosphorylation. Additionally, it impedes TGF-β1-induced migration and deforma... |
|
T72383 |
3,3-Dimethyl-1-butanol
|
Neohexanol,DMB,DMB ; Neohexanol |
|
|
3,3-Dimethyl-1-butanol (DMB) is an orally active compound that inhibits trimethylamine (TMA) and trimethylamine N-oxide (TMAO), along with the signaling pathways of p65 NF-κB and TGF-β1/Smad3. It holds potential for use ... |
|
T74996 |
FXR agonist 3
|
|
|
|
FXR agonist 3, an anti-NASH (Non-Alcoholic Steatohepatitis) agent, functions by activating FXR. It demonstrates anti-fibrogenic activity by inhibiting the expression of COL1A1, TGF-β1, α-SMA, and TIMP1. Additionally, it ... |
|
T61029 |
TP0427736 hydrochloride
|
|
|
|
TP0427736 hydrochloride can be used in the androgenic alopecia (AGA) research. TP0427736 hydrochloride inhibits the phosphorylation of Smad2/3 in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. TP0427736 hydr... |
|
T69990 |
Ruboxistaurin mesylate monohydrate
|
|
|
|
Ruboxistaurin mesylate monohydrate is a PKC beta inhibitor potentially for the treatment of diabetic nephropathy and diabetic macular edema. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/Smad and... |
|
T60854 |
ENMD-1068 hydrochloride
|
|
|
|
ENMD-1068 hydrochloride, a selective protease-activated receptor 2 (PAR2) antagonist, inhibits TGF-β1/Smad signaling, thereby reducing hepatic stellate cell activation and collagen expression. It also suppresses the prol... |
|
T82314 |
GK444
|
|
HDAC
|
|
GK444 (Compound 15a), a selective HDAC1/2 inhibitor with IC50 values of 100 nM and 92 nM for HDAC1 and HDAC2 respectively, demonstrates an IC50 of 4.1 μM in Caco-2 cell inhibition. Additionally, GK444 attenuates TGF-β1-i... |
|
T75716 |
Disitertide TFA
|
|
|
|
Disitertide (P144) TFA is a peptide-based inhibitor of transforming growth factor-beta 1 (TGF-β1), specifically engineered to prevent its interaction with the receptor. Additionally, it functions as a PI3K inhibitor and ... |
|
T21978 |
P-nitro-Pifithrin-α
|
|
|
|
p-nitro-Pifithrin-α is a cell-permeable analog of pifithrin-α, a potent p53 inhibitor. It suppresses p53-mediated TGF-β1 expression in HK-2 cells and inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. Mor... |
|
T75717 |
Disitertide diammonium
|
|
|
|
Disitertide (P144) diammonium, a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor, is specifically engineered to prevent its receptor interaction. Additionally, it serves as a PI3K inhibitor and induces apop... |
|
T63776 |
PDE1-IN-4
|
|
|
|
PDE1-IN-4 is a potent and selective inhibitor of PDE1 (phosphodiesterase-1), acting on PDE1C (IC50: 10 nM), PDE1A (IC50: 145 nM) and PDE1B (IC50: 354 nM). PDE1-IN-4 regulates cAMP (3′,5′-cyclic adenosine monophosphate) a... |
|
T83744 |
Tiger17 TFA
|
H-Trp-Cys-Lys-Pro-Lys-Pro-Lys-Pro-Arg-Cys-His-NH2 |
|
|
Tiger17, a cyclic peptide derivative of tigerinin-RC1 and tigerinin-RC2—antimicrobial peptides from the crab-eating frog (F. cancrivora) skin secretions—enhances HaCaT keratinocytes and human skin fibroblasts proliferati... |
|
T71884 |
ß-Carboline-1-carboxylic acid
|
|
|
|
β-Carboline-1-carboxylic acid is an alkaloid that has been found in P. quassioides and has diverse biological activities. It reduces LPS-induced increases in MCP-1, TNF-α, IL-6, and IL-1β levels in RAW 264.7 cells when u... |
|
T61585 |
Sulindac sodium
|
|
|
|
Sulindac (sodium) (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac (sodium) is used to reduce pain, swelling, and joint stiffness from arthritis. Sulindac is also used for the research of arthr... |
