tgf-β

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

GSK-J4 (GSK J4 HCl) is a cell permeable prodrug of GSK-J1, a dual inhibitor of the H3K27me3/me2 demethylases JMJD3/KDM6B and UTX/KDM6A (IC50=8.6/6.6 μM). GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

CJJ300 is a transforming growth factor-β (TGF-β) inhibitor with an IC50 of 5.3 μM, disrupting the TGF-β-TβR-I-TβR-II signaling complex and inhibiting cell migration.

NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor that disrupts the [SIX1/EYA2] complex, EMT, and metastasis.

Ogerin is a selective GPR68 positive allosteric modulator (pEC50: 6.83) that blocks recall in fear conditioning in mice. It exhibits inverse agonist and antagonist activity (Ki, 220 nM) at the A2A receptor and weak antagonist activity (Ki, 736 nM) at the 5-HT2B receptor.

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.

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

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

GSK-J4 Hydrochloride (GSK J4 HCl) is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro.

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.

Gnetol competitivity inhibits butyrylcholinesterase (IC50: 1.3 uM). Gnetol has a strong inhibitory effect on murine tyrosinase activity. Gnetol significantly suppresses melanin biosynthesis in murine B16 melanoma cells. It is active in the inhibition of a

HALOFUGINONE LACTATE is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity

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 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.

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.

SB-431542 is an inhibitor of ALK5/TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.

LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8/0.8/5.3/16.7 nM for ALK1/2/3/6).

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

Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity.

Pirfenidone (AMR69) inhibits the production of CCL2 and CCL12 in fibroblasts and also decreases TGF-β2 protein levels. Pirfenidone is an antifibrotic agent that is commonly used in studies related to pulmonary fibrosis and also has anti-inflammatory activity.

Galunisertib (LY2157299) is a TGF-β receptor type I (TGF-βRI) inhibitor (IC50=56 nM) that is selective. Galunisertib has antitumor activity and can be used in combination with PD-1 inhibitors.

Monocrotaline is an 11-membered macrocyclic pyrrolizidine alkaloid extracted from the seeds of Crotalaria plants. It inhibits organic cation transporters OCT-1 and OCT-2, with IC50 values of 36.8 µM and 1.8 mM, respectively. Monocrotaline exhibits antitumor activity and shows certain cytotoxicity against liver cancer cells such as HepG2. It is also commonly used to induce pulmonary arterial hypertension models in rodents.