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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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. |
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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. |
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V7153 | A83-01 | 909910-43-6 | A-83-01 is an ALK inhibibitor. |
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V51372 | ALK2-IN-4 | 2248154-85-8 | ALK2-IN-4 is an effective ALK2 inhibitor. |
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V51373 | ALK2-IN-4 succinate | 2416307-25-8 | ALK2-IN-4 succinate is an effective ALK2 inhibitor. |
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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. |
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V3313 | BIBF0775 | 334951-90-5 | BIBF0775, a 6-substituted indolinone analog, is a novel, potent and selective inhibitor oftransforming growth factor β (TGFβ) type I receptor (Alk5)with anIC50of 34 nM. |
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V67592 | Bimagrumab (Anti-ACVR2B Reference Antibody; BYM338) | 1356922-05-8 | Bimagrumab (Anti-ACVR2B Reference Antibody) is a human monoclonal antibody (mAb) that blocks activin type II receptor (ActRII) with Kds of 1.7 pM for ActRIIB and 434 pM for ActRIIA. |
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V67574 | Bintrafusp alfa (M7824; MSB0011359C) | 1918149-01-5 | Bintrafusp alfa (M 7824) is a first-in-class bifunctional fusion protein consisting of the extracellular domain of TGF-βRII fused to a human IgG1 mAb blocking programmed cell death ligand. |
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V12686 | BIO-013077-01 | 746667-48-1 | BIO-013077-01 is a pyrazole-based TGF-β inhibitor. |
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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. |
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V80273 | BMPR2-IN-1 | MPR2-IN-1 (Compound 8a) is a BMPR2 inhibitor (antagonist) with IC50 of 506 nM and a KD of 83.5 nM. | |
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V51269 | Dalutrafusp alfa (AGEN-1423; GS-1423) | 2419918-89-9 | Dalutrafusp alfa (AGEN-1423; GS-1423) is a specific anti-CD73 and TGF-β bifunctional antibody that participates in immunosuppressive pathways. |
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V67568 | Garetosmab (REGN 2477) | 2097125-54-5 | Garetosmab (REGN 2477) is a fully human IgG4 monoclonal antibody (mAb) that specifically inhibits activin A. |
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V67573 | Isosaponarin | 19416-87-6 | Isosaponarin is a flavonoid glycoside extracted from mustard leaves that can increase collagen synthesis, which is caused by up-regulation of TGF-β type II receptor (TβR-II) and prolyl 4-hydroxylase ( Caused by the production of P4H) protein. |
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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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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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