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 |
|---|---|---|---|---|
|
V121284 | (14S,15R)-14-Deoxyoxacyclododecindione | 1899061-36-9 | (14S,15R)-14-deoxyoxecyclic dodecenedione (compound 3) inhibits TGF-β-dependent Smad2/3 and IL-4-dependent STAT6, with IC50 values of 90 nM and 20 nM, respectively. |
|
V67588 | A 83-01 sodium | 2828431-89-4 | A 83-01 sodium is a potent inhibitor of TGF-β type I receptors ALK5, ALK4 and ALK7. |
|
V7118 | A77-01 | 607737-87-1 | A 77-01 is a potent inhibitor of the TGF-β type I receptor family ALK5 with IC50 of 25 nM. |
|
V7153 | A83-01 | 909910-43-6 | A-83-01 is an ALK inhibibitor. |
|
V128263 | ActRIIB-IN-1 | 3039974-31-4 | ActRIIB-IN-1 is an orally effective activin type II receptor B (ActRIIB) inhibitor with an IC50 value of 1.8 nM. |
|
V128264 | ActRIIB-IN-2 | 3039974-32-5 | ActRIIB-IN-2 is an ActRIIB inhibitor with an IC50 of 1.1 nM. |
|
V128265 | ActRIIB-IN-3 | 3039974-35-8 | ActRIIB-IN-3 is an ActRIIB inhibitor. |
|
V128266 | ActRIIB-IN-4 | 3039974-41-6 | ActRIIB-IN-4 is an ActRIIB inhibitor with an IC50 of 4.0 nM. |
|
V85086 | ALK-5-IN-1 | 1018953-58-6 | |
|
V51372 | ALK2-IN-4 | 2248154-85-8 | ALK2-IN-4 is an effective ALK2 inhibitor. |
|
V51373 | ALK2-IN-4 succinate | 2416307-25-8 | ALK2-IN-4 succinate is an effective ALK2 inhibitor. |
|
V114630 | ALK2-IN-6 | 2600795-23-9 | ALK2-IN-6 (compound 14a) is a selective ALK2 inhibitor with an IC50 of 9 nM. |
|
V83494 | ALK5-IN-10 | 1352608-94-6 | |
|
V88165 | ALK5-IN-80 | ALK5-IN-80 (Compound 29b) is a selective ALK5 inhibitor with IC50 of 3.7 nM. | |
|
V118263 | ALK5-IN-85 | 2766583-86-0 | ALK5-IN-85 (compound 19) is a TGFβRI (ALK5) inhibitor with IC50 < 100 nM. |
|
V128811 | ANB012 | ANB012 is an antibody targeting human ACVR2B. | |
|
V129671 | Autotaxin-IN-7 | Autotaxin-IN-7 is a pyridine-2-carboxylic acid derivative with sub-nanomolar ATX inhibitory activity (IC50 = 0.086 nM), good cardiac safety (hERG > 30 μM), and extremely low fibroblast toxicity. | |
|
V67589 | AZ12601011 | 2748337-86-0 | AZ12601011 is an orally bioactive, selective TGFBR1 kinase inhibitor (antagonist) with IC50 of 18 nM and a Kd of 2.9 nM. |
|
V106422 | Bezeotermin alfa | Bezeotermin alfa is a fusion protein targeting BMP-6. | |
|
V118413 | BI-4659 | 894784-05-5 | BI-4659 (compound 47i) is a TGF-β type I receptor (TGF-βRI (Alk5)) inhibitor with an IC50 of 19 nM. |
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