tgf-β1

Methacycline hydrochloride (Rondomycin) is a broad-spectrum semisynthetic antibiotic related to TETRACYCLINE but excreted more slowly and maintaining effective blood levels for a more extended period.

TGF-β1/Smad3-IN-1 (Compound 5aa) is an inhibitor of the TGF-β1/Smad3 signaling pathway, with an IC50 value of 1.07 μM. It exhibits anti-fibrotic properties and is effective orally.

Cassiaside C (Toralactone 9-O-β-D-gentiobioside), a naphthopyrone extracted from Cassia tora seeds, demonstrates in vitro inhibitory activity against the formation of advanced glycation end products (AGE).

Flavanomarein demonstrates potent antioxidative property, including free radical scavenging activity, inhibition of lipid peroxidation, as well as lipid-lowering effects in human HepG2 hepatocellular carcinoma cells treated with free fatty acids (FFAs).

LSKL TFA (H-Leu-Ser-Lys-Leu-NH2 TFA) is a LAP-TGFβ derivative and a TGF-β1 antagonist that can cross the blood-brain barrier, inhibits the binding of TSP-1 to LAP and reduces renal interstitial fibrosis and liver fibrosis, inhibits subarachnoid fibrosis by inhibiting TSP-1-mediated TGF-β1 activity, prevents the occurrence of chronic hydrocephalus and improves long-term neurocognitive deficits after subarachnoid hemorrhage.

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] [2].

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 the ability to attract neutrophils [1] [2].

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 apoptosis inducer.

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 TGF-β1-induced activation of fibroblasts in vitro, inhibits activation of macrophages and fibroblasts, and inhibits scarring in wound healing models.

AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 of 1.6 nM and a Kd of 0.26 nM. It exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion.

Disitertide (P144) is an inhibitor of TGF-β1.

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 of Wnt target genes, and promotes apoptosis in cancer cells, displaying anti-cancer properties. Furthermore, it functions as an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM.

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

Isoviolanthin reduces the migratory and invasive capacities of TGF-β1-treated HCC cells without cytotoxic effects on normal live cells and has potential as a therapeutic agent for the treatment of advanced-stage metastatic HCC. Isoviolanthin is a flavonoid glycoside extracted from the leaves of Dendrobium Officinale.

SB-525334 is a potent and selective inhibitor of the TGF-β1R and ALK5 (IC50: 14.3 nM).

JNK-1-IN-4 (Compound E1) is an inhibitor of JNK, targeting JNK-1, JNK-2, and JNK-3 with IC50 values of 2.7, 19.0, and 9.0 nM, respectively. This compound inhibits the phosphorylation of c-Jun and reduces the expression of TGF-β1-induced EMT markers (such as fibronectin and α-SMA). JNK-1-IN-4 exhibits favorable pharmacokinetic properties with a bioavailability of 69%. Additionally, it demonstrates antifibrotic effects in a Bleomycin-induced mouse model of idiopathic pulmonary fibrosis.

ALK5-IN-83 (compound 13b) is an ALK5 inhibitor with an IC50 of 0.13 μM. It suppresses TGF-β1-induced Smad2 phosphorylation and cell motility in A549 cells.

STAT3-IN-39 (compound 10K) is an orally active inhibitor of STAT3, demonstrating effective inhibition of STAT3 phosphorylation with an IC50 of 0.47 μM in NIH-3T3 cells. It hinders TGF-β1-induced fibrotic responses and prevents epithelial-mesenchymal transition in A549 cells. STAT3-IN-39 is applicable for research related to idiopathic pulmonary fibrosis.

MORF-627 is an orally active selective inhibitor of integrin αvβ6 (integrinαvβ6), with an IC50 of 9.2 nM as measured in a human serum ligand binding assay. It effectively inhibits αvβ6-mediated activation of TGF-β1 with an IC50 of 2.63 nM and suppresses SMAD2/3 phosphorylation, showing an IC50 of 8.3 nM. Additionally, MORF-627 ameliorates bleomycin-induced pulmonary fibrosis in mice.

PROTAC AR Degrader-9 (Compound c6) is a PROTAC-based degrader specifically targeting the androgen receptor. It effectively degrades the androgen receptor in human dermal papilla cells (HDPC) with a DC50 of 262.38 nM. Additionally, this compound enhances the expression of paracrine factors, such as TGF-β1 and β-catenin, thereby promoting hair regeneration in mouse models. [Pink: ligand for target protein AR ligand-38; Black: linker; Blue: ligand for E3 ligase Cereblon]

NOX4-IN-1 (Compound 14m) is an inhibitor of NADPH oxidase 4 (NOX4) that reduces the production of reactive oxygen species (ROS). It also inhibits the TGF-β1/Smad signaling pathway, leading to decreased expression of fibrosis-related proteins. Additionally, NOX4-IN-1 impedes the migration of NRK-49F cells.

FGFRs-IN-1 (Compound A16) is an orally active inhibitor targeting FGFR1/2/3/4, with IC50 values of 2.3, 7, 11, and 163 nM respectively. It also inhibits VEGFR1/2/3, Abl, and Flt3, with IC50 values of 61, 176, 112, 26, and 353 nM. The compound shows weak inhibition of CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and it inhibits epithelial-mesenchymal transition (EMT) in A549 cells stimulated by TGF-β1. Additionally, FGFRs-IN-1 demonstrates anti-inflammatory activity in mouse models of lung fibrosis induced by Bleomycin and liver fibrosis induced by CCl4.

HDAC6-IN-53 (Compound W28) is an inhibitor targeting histone deacetylase 6 (HDAC6) with an IC50 of 19.65 nM. It reduces the idiopathic pulmonary fibrosis (IPF) phenotype by inhibiting TGF-β1-induced collagen expression and demonstrates therapeutic efficacy in a bleomycin-induced mouse model of pulmonary fibrosis. HDAC6-IN-53 is applicable for research in idiopathic pulmonary fibrosis and related pulmonary fibrotic diseases.

TRPC6 antagonist-1 (X26) is a TRPC6 inhibitor with IC50 values of 0.97 μM for TRPC6, 3.93 μM for TRPC3, 5.77 μM for TRPC5, and 4.37 μM for TRPC7. Additionally, TRPC6 antagonist-1 hinders TGF-β1-induced myofibroblast differentiation, thereby mitigating renal fibrosis.