transforming growth factor-β

Estramustine phosphate sodium (Ro 21-8837/001) is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.

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.

A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12/45/7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.

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

RepSox (ALK5 Inhibitor II) is a TGFβR-1/ALK5 inhibitor that selectively inhibits the binding of ATP to ALK5 and the autophosphorylation of ALK5 (IC50=23/4 nM). RepSox induces adipogenesis in MEFs cells.

BMP signaling agonist sb4 (SB 4) is an agonist of benzoxazole bone morphogenetic protein (BMP) signaling (EC50 :74 nM)

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.

Hydrochlorothiazide (HCTZ) is a Thiazide Diuretic. The physiologic effect of hydrochlorothiazide is by means of Increased Diuresis.

Oxymatrine (Oxysophoridine) is an alkaloid isolated from Sophora flavescens, used as the antibiotic. It is a traditional Chinese medicine used in the treatment against hepatitis B virus.It can also inhibit iNOS expression and TGF - β / Smad pathway.

Alantolactone is a selective inhibitor of STAT3 that induces cancer-associated apoptosis and has antitumor activity.

Maohuoside A promotes osteogenesis of rat mesenchymal stem cells via BMP and MAPK signaling pathways.

CDDO-dhTFEA, a synthetic oleanane triterpenoid, effectively activates Nrf2 while inhibiting the NF-κB pro-inflammatory transcription factor. It restores mean arterial pressure (MAP), elevates Nrf2 levels and the expression of related genes, attenuates NF-κB and transforming growth factor-β pathway activation, and mitigates glomerulosclerosis, interstitial fibrosis, and inflammation in rats with chronic kidney disease (CKD).

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.

Kartogenin (KGN) is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.

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

GW788388 is a potent and selective inhibitor of ALK5, and it also inhibits TGF-(beta) type II receptor and activin type II receptor activities.

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.