tgf-β 3

TGF-βRI inhibitor 3 (Compound 9ac) is a selective inhibitor of TGF-β that effectively suppresses the TGF-β signaling pathway. It exhibits IC50 values of 13 μM for c-Src kinase and 0.63 μM for ALK5 kinase.

TGF-β1/Smad3-IN-1 (Compound 5aa) is an orally administrable dual inhibitor of TGF-β1/Smad3 with anti-fibrotic activity and can be used for the study of idiopathic pulmonary fibrosis (IPF).

SIS3 free base is a potent and selective inhibitor of Smad3 phosphorylation, effectively inhibiting the TGF-β1-induced myofibroblast differentiation of fibroblasts.

LDN-212854 (BMP Inhibitor III), 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 ALK1/3 compared to other inhibitors.

GED-0507-34 Levo ((S)-3-(4-Aminophenyl)-2-methoxypropanoic acid), an orally available PPARγ modulator for amelioration of inflammation-driven intestinal fibrosis, decreased the expression of the pro-fibrotic genes Acta2, COL1a1, and Fn1, reduced the protein levels of α-SMA and collagen I-II, the main markers of fibrosis, as well as the major components of the TGFβ/Smad pathway, and decreased the expression of IL-13, CTGF, TGFB and ACTA1, and inhibited TGF-β-induced activation of fibroblasts and IECs cell lines.

Dual Galectin-3/EGFR-IN-1 (Compound 29) is a dual inhibitor targeting Galectin-3 and EGFR, with dissociation constants (KD) of 52.29 μM and 3.31 μM, respectively. It inhibits TGF-β-induced hepatic stellate cell (HSC) activation, induces apoptosis in LX-2 cells, and shows antifibrotic activity in the liver.

TRPV1-IN-3 (compound 14) is a TRPV1 inhibitor utilized in idiopathic pulmonary fibrosis research. It demonstrates antifibrotic activity in vitro (IC50 = 0.51 μM) by inhibiting the TGF-β/Smads and MAPK pathways, thereby affecting the expression of fibrosis markers collagen I and α-SMA. In vivo, TRPV1-IN-3 significantly reduces collagen deposition in lung tissue, improves alveolar structure, and increases survival rates in mice with Bleomycin-induced pulmonary fibrosis.

Smad2/3-IN-2 (Compound 3) is an inhibitor of the TGF-β-dependent Smad2/3 signaling pathway and the IL-4-dependent STAT6 signaling pathway, with IC50 values of 90 nM and 20 nM, respectively.

Smad2/3-IN-2 (Compound 27) is an inhibitor of the TGF-β-dependent Smad2/3 signaling pathway and the IL-4-dependent STAT6 signaling pathway, with IC50 values of 90 nM and 20 nM, respectively.

TTTE is a sulfone-bischalcone derivative with primary activities including anti-hepatic necrosis, anti-inflammatory, and anti-fibrotic effects. It modulates these activities by downregulating key molecules such as Caspase-3, TNF-α, NF-κB, and TGF-β. TTTE can be utilized in the study of liver injury.

Butaprost is a selective agonist of the prostaglandin E receptor EP2 that exhibits an EC50 of 33 nM and a Ki of 2.4 μM toward the murine EP2 receptor, while showing markedly lower activity against murine EP1, EP3, and EP4 receptors. Butaprost effectively attenuates fibrotic responses by inhibiting the TGF-β/Smad2 signaling pathway, supporting its utility in fibrosis, inflammation, and prostaglandin receptor signaling research.

Lipoxygenin is an inhibitor of 5-lipoxygenase (5-LO) with an IC50value of 5 μM for inhibition of 5-LO product synthesis in isolated human granulocytes stimulated with the cation ionophore A23187 .1It inhibits hedgehog-dependent signaling in Shh-LIGHT2 cells and TGF-β-, activin A-, bone morphogenic protein (BMP)-, or Wnt-dependent signaling in HEK293T cells (IC50s = 9.3, 3.2, 8.2, 9.6, and 3.7 μM, respectively, in luciferase reporter assays). Lipoxygenin (5 and 10 μM) increases levels of troponin T (TnnT), a marker of cardiomyocyte differentiation, in human induced pluripotent stem cells (iPSCs) stimulated with BMP4 and the glycogen synthase kinase 3 (GSK3) inhibitor CHIR99021 .

(E)-SIS3 (SIS3) is a Smad3 inhibitor (IC50=3 μM) and is selective. (E)-SIS3 inhibits the differentiation of fibroblasts into myofibroblasts via TGF-β1.

TP0427736 hydrochloride is a novel and selective ALK5 inhibitor with an IC50 of 2.72 nM, capable of inhibiting Smad2/3 phosphorylation in A549 cells, reducing TGF-β-induced growth inhibition of human root sheath cells, and prolonging the anagen phase of mouse hair follicles.

H-Gly-Pro-Hyp-OH is a potent and orally available anti-photoaging collagen peptide that attenuates inflammation and reduces MMP-1 and MMP-3 levels; attenuates H2O2-induced aging of dermal fibroblasts; restores cortisol-mediated inhibition of type I collagen and GR activation and (TGF)-β signaling signaling, among other things; and improves the hydration of human skin, elasticity and anti-wrinkle properties.

BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).

2-APQC is a selective, orally active Sirtuin-3 (SIRT3) agonist (Kd=2.756 μM) that modulates mitochondrial homeostasis. It attenuates ISO-induced myocardial hypertrophy and fibrosis in vivo and in vitro, making it suitable for heart failure research. 2-APQC inhibits mTOR-p70S6K, JNK, TGF-β/Smad3, and ROS-p38MAPK pathways while activating PYCR1 and AMPK-Parkin, thereby suppressing necrosis and mitigating mitochondrial oxidative damage.

sTGFBR3 antagonist 1 (Compound p24) is an antagonist of soluble transforming growth factor β receptor 3 (sTGFBR3) that activates the TGF-β signaling pathway while inhibiting the IκBα/NF-κB signaling pathway. It inhibits the release of NO induced by LPS in BV2 cells with an IC50 of 0.52 μM. sTGFBR3 antagonist 1 exhibits anti-inflammatory and neuroprotective activities and can enhance the permeability of the blood-brain barrier (BBB). This compound is applicable in research related to Alzheimers disease.

TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor with an IC50 of 0.79 nM and exhibits 2000-fold selectivity against MAP4K4, showing potential applications in immuno-oncology [1].

Anti-INHBB/Activin B Antibody is a monoclonal antibody specifically targeting the inhibin subunit beta B (INHBB). The INHBB subunit homodimerizes to form Activin B, a member of the TGF-β superfamily involved in regulating cell proliferation, differentiation, apoptosis, and various pathological processes. By specifically binding to INHBB, this antibody blocks the interaction of Activin B with its receptors (e.g., ActRIIA/B and ALK4/7), thereby inhibiting the activation of the Smad2/3 signaling pathway. In experimental research, this antibody is frequently utilized to study liver fibrosis, muscle wasting (cachexia), and the progression mechanisms of various tumors.

Isoangustone A is a natural product that inhibits PI3K, MKK4, and MKK7 through ATP competition, suppresses the expression of G1 phase regulatory proteins, inhibits the phosphorylation of Akt, GSK-3β, and JNK1/2, and inhibits the proliferation of human melanoma cells and tumour growth in xenograft mouse models.

Klotho-derived peptide 1 (KP1 human) hydrochloride inhibits the interaction between TGF-β and TGF-β receptor 2, suppressing the activation of TGF-β-induced Smad2/3 and mitogen-activated protein kinase (MAPK). Additionally, it exhibits antifibrotic and renal protective effects in mouse models.

Klotho-derived peptide 1 (KP1 human) can inhibit the interaction between TGF-β and its receptor TGF-β receptor 2, suppressing the activation of Smad2/3 and mitogen-activated protein kinase (MAPK) induced by TGF-β. It shows anti-fibrotic and renal protective effects in mouse models.