Single pass serine/threonine kinase receptors are TGF-Rs, or transforming growth factor receptors. Transforming growth factor beta (TGF-beta) is a pleiotropic cytokine that participates in a wide range of biological functions, including the regulation of growth, differentiation, migration, cell survival, adhesion, and the specification of developmental fate, in both healthy and pathological conditions. Members of the TGF-beta superfamily communicate via a receptor complex made up of type II and type I receptors, both of which are serine/threonine kinases.At the center of the signaling cascade, the type I receptors, also known as activin receptor-like kinases (ALK), transmit TGF-beta signals to Smad proteins, which are intracellular transcriptional regulators.
ALKs have extracellular binding domains, transmembrane domains, GS domains that type II receptors use to activate them, and kinase domains that trigger the activation of subsequent signaling molecules. ALKs mediate the effect of TGF-beta superfamily on a variety of cellular processes such as proliferation, differentiation, apoptosis, adhesion and migration, and therefore play important roles in many biological processes. ALKs may make good drug targets because they have been linked to a variety of diseases, including tumorigenesis and immune disorders.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V67579 | TGFβRI-IN-6 | 2072051-04-6 | TGFβRI-IN-6 is a potent inhibitor of TGFβRI with IC50 of 0.55 nM. |
|
V67590 | THRX-144644 | 2442519-59-5 | THRX-144644 is a lung-restricted ALK5 inhibitor (antagonist) with IC50 of 0.14 nM. |
|
V20870 | Vactosertib (EW-7197) Hydrochloride | 1352610-25-3 | Vactosertib HCl (formerly EW-7197; EW7197) is a highly potent, selective, and orally bioavailable inhibitor of the TGF-β receptor ALK4/ALK5 with anticancer and immunomodulatory effects. |
|
V3262 | Vactosertib (EW7197; TEW7197) | 1352608-82-2 | Vactosertib (formerly EW-7197; TEW-7197)is a highly potent, selective, ATP-competitive and orally bioavailable inhibitor of the TGF-β receptor ALK4/ALK5 (activin receptor-like kinase) with potential anticancer activity. |
|
V67583 | Vicatertide (SB-01) | 1251838-01-3 | Vicatertide is a TGF beta-1 inhibitor. |
|
V67587 | Zilurgisertib (INCB-000928; NBU-928) | 2173389-57-4 | Zilurgisertib (INCB-000928; NBU-928) is a selective ALK 2 inhibitor used to study diseases like cancer. |
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