transforming growth factor β 1

DMH-1 is a potent and selective Bone Morphogenetic Protein (BMP) inhibitor.

SRI-011381 hydrochloride, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.

5Z-7-Oxozeaenol (FR148083) is a potent, irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 with IC50 of 8.1 nM for TAK1 and low activity against MEK1 with IC50 of 411 nM, it is also an inhibitor of VEGF-R2 with IC50 of 52 nM.

Pelubiprofen is an orally active, non-steroidal anti-inflammatory agent, a selective cyclooxygenase-2 (COX-2) inhibitor, which effectively reduces PGE(2) production by inhibiting COX activity. Pelubiprofen inhibits LPS-induced phosphorylation of IKK-β and transforming growth factor-β activated kinase-1 (TAK1).

R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor.

ALK5-IN-82 is a potent and selective inhibitor of activin receptor-like kinase 5 (ALK5), demonstrating an IC50 value of 9.1 nM. This compound effectively suppresses the expression of α-smooth muscle actin (α-SMA), collagen I, and the proteinases tissue inhibitor of metalloproteinase 1 (TIMP-1) and matrix metalloproteinase 13 (MMP-13) in human umbilical vein endothelial cells induced by transforming growth factor-β. ALK5-IN-82 shows potential for use in research related to cardiac fibrosis.

ITD-1 is a potent and highly selective TGFβ pathway inhibitor.

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. It also inhibits the PDGFR, EGFR, and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively.

(5E)-7-Oxozeaenol is a resorcylic acid lactone that has been found in the fungus MSX 63935 and has enzyme inhibitory and anticancer activities.1,2 It inhibits TGF-β-activated kinase 1 (TAK-1; IC50 = 1.3 μM).1 (5E)-7-Oxozeaenol inhibits proliferation of MCF-7, H460, SF-268, HT-29, and MDA-MB-435 human cancer cells with IC50 values of 4.9, 1.2, 5.6, 4.4, and 5.5 μM, respectively.2 |1. Fakhouri, L., El-Elimat, T., Hurst, D.P., et al. Isolation, semisynthesis, covalent docking and transforming growth factor beta-activated kinase 1 (TAK1)-inhibitory activities of (5Z)-7-oxozeaenol analogues. Bioorg. Med. Chem. 23(21), 6993-6999 (2015).|2. Ayers, S., Graf, T.N., Adcock, A.F., et al. Resorcylic acid lactones with cytotoxic and NF-κB inhibitory activities and their structure-activity relationships. J. Nat. Prod. 74(5), 1126-1131 (2011).

SRI-011381, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.

TGFβ-IN-1 is an antitumor growth and metastasis agent that functions by inhibiting the transforming growth factor β (TGFβ) signaling pathway.

Halofuginone (RU-19110), the competitive inhibitor of prolyl-tRNA synthetase(Ki=18.3 nM), could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng ml in the mammal.

Chlorfortunone A, a novel sesquiterpenoid dimer isolated from the roots of Chloranthus fortunei, inhibits transforming growth factor (TGF)-β activity [1].

Luspatercept (ACE-536), a recombinant modified ActRIIB fusion protein, selectively binds to transforming growth factor β superfamily ligands, thereby enhancing erythrocyte production and advancing the maturation of erythroid precursors. Moreover, by binding with GDF11, it inhibits Smad2 3 signaling. This compound is instrumental in anemia research [1].

Pentabromopseudilin (PBrP), a marine antibiotic derived from Pseudomonas bromoutilis and Alteromonas luteoviolaceus, demonstrates antimicrobial, antitumor, and phytotoxic properties. It acts as a reversible, allosteric inhibitor of myosin Va (MyoVa) and robustly inhibits transforming growth factor-β (TGF-β) activity. PBrP is utilized in researching fibrotic diseases and cancer [1].

J27644 is a potent HDAC (histone deacetylase) inhibitor that mitigates TGF-β (transforming growth factor beta)-induced pulmonary fibrosis [1].

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.

IMM-H007 is a novel lipid-lowering agent, increasing abca1 protein expression