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 |
|---|---|---|---|---|
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V3756 | LY3200882 | 1898283-02-7 | LY3200882 is a next generation,ATP competitive, potent, highly selective small molecule inhibitor of TGF-β receptor type 1 (TGFβRI). |
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V67584 | Maohuoside A | 128988-55-6 | Maohuoside A, a single compound extracted from E. |
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V67582 | Metelimumab (CAT-192; Anti-TGFB1 Recombinant Antibody) | 272780-74-2 | Metelimumab (CAT-192) is a human IgG4 monoclonal antibody (mAb) that selectively neutralizes TGFβ1. |
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V78829 | MU1700 | MU1700 is an orally bioactive, potent ALK1/2 inhibitor (antagonist) with IC50s of 13 nM and 6 nM, respectively, which is cell membrane permeable (penetrable) and has high brain permeability. | |
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V76721 | Nadecnemab | Nadecnemab is an IgG4κ antibody targeting the glial cell-derived neurotrophic factor family receptor GFRA3. | |
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V67586 | Pentabromopseudilin | 10245-81-5 | Pentabromopseudilin (PBrP) is a marine antibiotic extracted from the marine bacteria Pseudomonas bromoutilis and Alteromonas luteoviolaceus. |
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V67585 | Ramatercept | 1169766-01-1 | Ramatercept is a soluble ActRIIB receptor that works as a soluble activin receptor 2 (ACVR2) antagonist. |
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V12277 | SB-505124 HCl | 356559-13-2 | SB-505124 HCl, the hydrochloride salt ofSB505124, is a selective inhibitor of TGFβR (TGF-β Receptor type I receptor) for ALK4, ALK5 (activin receptor-like kinase) with potential anticancer activity. |
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V67572 | SHR-1701 (Retlirafus alfa) | 2891860-17-4 | SHR-1701 (Retlirafusp alfa) is a bifunctional fusion protein targeting PD-L1 and TGFβ and may be utilized in cancer-related research. |
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V4040 | SJ000291942 | 425613-09-8 | SJ000291942 is anew small-molecule activator of the canonical BMP (bone morphogenetic proteins) signaling pathway. |
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V14105 | SM16 | 614749-78-9 | SM16 is a novel and potent Type I TGF-β signaling inhibitor, also a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively. |
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V67593 | Sotatercept (ACE-011) | 1001080-50-7 | Sotatercept (ACE-011) is a soluble activin receptor 2A (ACVR2A)-type IgG Fc fusion protein. |
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V67581 | Stamulumab (MYO-029) | 705287-60-1 | 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. |
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V67577 | TGFβ-IN-1 | 883560-84-7 | TGFβ-IN-1 works as an anti-tumor growth and metastasis agent by inhibiting the transforming growth factor β signaling pathway. |
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V67580 | TGFβ-IN-5 | 259870-32-1 | TGFβ-IN-5 (Compd 12) is a TGFβ inhibitor that may be utilized in the study of fibroproliferative diseases related to TGF-β signal transduction. |
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V67570 | TGFβ1-IN-1 | 2348795-14-0 | TGFβ1-IN-1 (compound 42) is a potent, orally bioactive TGF-β1 inhibitor. |
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V67576 | TGFβ1-IN-2 | 2883813-66-7 | TGFβ1-IN-2 is a diarylacylhydrazone analogue that effectively inhibits fibroblast activation and proliferation. |
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V67575 | TGFβ1-IN-3 | 2883813-58-7 | TGFβ1-IN-3 is a diarylacylhydrazone analogue that effectively inhibits fibroblast activation and proliferation. |
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V67571 | TGFβR-IN-1 | 2857845-36-2 | TGFβR-IN-1 is the precursor of a long-acting tumor-activated TGFβR inhibitor. |
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V67569 | TGFβRI-IN-3 | 2763602-67-9 | TGFβRI-IN-3 inhibits TGFβR1 with IC50 of 0.79 nM and is 2000 times more selective than MAP4K4. |
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