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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V84595 | Itacnosertib (hydrocholide) (TP-0184 (hydrocholide)) | 2409543-84-4 | |
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V22771 | ITD-1 | 1099644-42-4 | ITD-1 is a selective inhibitor of TGF-β signaling (IC50 = 0.85 μM); exhibits little or no inhibition of activin, Wnt or BMP signaling pathways. |
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V87102 | J-1149 | 2883580-95-6 | J-1149 is a potent ALK5 inhibitor with an IC50 value of 0.017 μM. |
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V106344 | KQFK | 162290-88-2 | KQFK is an inactive control for KRFK, a TSP-1-derived peptide that activates TGF-β. |
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V67578 | KRFK | 162290-78-0 | KRFK is a bioactive peptide extracted from TSP-1 and can activate TGF-β. |
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V76847 | KRFK TFA | KRFK TFA is a bioactive peptide extracted from TSP-1 and can activate TGF-β. | |
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V67567 | LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) (LSKL, Inhibitor of Thrombospondin (TSP-1) trifluoroacetate) | 2828433-17-4 | LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a tetrapeptide extracted from LAP-TGFβ and is a competitive TGF-β1 antagonist. |
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V31090 | LSKL, Inhibitor of Thrombospondin TSP-1 | 283609-79-0 | LSKL is a potent and peptide-based inhibitor of Thrombospondin TSP-1 with the potential to be used for treatinghypertrophic scar. |
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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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V98117 | LY550410 | 737791-20-7 | LY550410 is a small molecule ATP-competitive type I TGF-β receptor kinase inhibitor with a heteroaromatic ring that effectively binds to the active site of the kinase domain. |
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V84758 | M4K2163 dihydrochloride | 2863635-04-3 | |
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V88161 | M4K2281 | M4K2281 is a selective inhibitor of activin receptor-like kinase 2 (ALK2) with IC50 of 2 nM. | |
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V88166 | M4K2306 | 3034840-25-7 | M4K2306 is a selective inhibitor of activin receptor-like kinase 2 (ALK2) with IC50 of 7 nM. |
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V67584 | Maohuoside A | 128988-55-6 | Maohuoside A, a single compound extracted from E. |
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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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V84564 | OXA-06 hydrochloride | 1825455-91-1 | |
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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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V86176 | PKA Substrate | 121932-31-8 | |
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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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V37829 | BMP signaling agonist sb4 | 100874-08-6 | BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with EC50 of 74 nM and activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. |