TGF-β Receptor

SM 16 is a ALK5/ALK4 kinase inhibitor

LSKL, Inhibitor of Thrombospondin TSP-1 is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin TSP-1 inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin TSP-1 suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin TSP-1 can readily crosse the blood-brain barrier.

A BMP signaling activator

R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM.

BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.

A potent inhibitor of TGF-β type I receptor ALK5 kinase

A selective BMP type I receptor inhibitor

Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect.

LSKL, Inhibitor of Thrombospondin TSP-1, is a tetrapeptide derived from Latency-Associated Protein (LAP)-TGFβ. LSKL competitively binds to and inhibits TGF-β1.

N-Acetylpuromycin is a non-ribotoxic form of the antibiotic puromycin that is formed in puromycin-resistant S.

Potent and selective inhibitor of TGF-βRI

Potent TGF-βRI inhibitor

SB-4 is a potent benzoxazole Bone morphogenetic protein 4 (BMP4) signaling agonist with an EC 50 value of 73.64nM.

Isosaponarin is a flavone glycoside isolated from wasabi leaves.

XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.

BIO-013077-01 is a pyrazole TGF-β inhibitor.

ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.

EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung.

Fresolimumab is a high-affinity humanized monoclonal antibody that binds to and inhibits all isoforms of the protein transforming growth factor β (TGFβ). The K d values of Fresolimumab for TGFβ1, TGFβ2, and TGFβ3 are 1.7±0.6nM, 3.0±1.2nM, and 2.0±1.2nM, respectively.

TGFβ1-IN-1 is a highly effective, orally active transforming growth factor β1 (TGF-β1) specific inhibitor that can significantly block the TGF-β1 signaling pathway and inhibit the upregulation of fibrosis-related proteins (such as α-smooth muscle actin and fibronectin) mediated by it. It is suitable for the mechanism research and treatment development of fibroproliferative diseases such as liver fibrosis.

Chromenone 1 is a potent osteogenic bone morphogenetic protein (BMP) potentiator.

KRFK TFA, a peptide derived from TSP-1, can activate TGF-β.

Vicatertide is a TGF beta-1 inhibitor.

Stamulumab (MYO-029) is a recombinant human IgG1λ antibody that binds to myostatin and neutralizes its activity by preventing binding to its endogenous high-affinity receptor ActRIIB.