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TGF-β Receptor

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TGF-β receptors (Transforming growth factor-β receptors) are single pass serine/threonine kinase receptors. Transforming growth factor beta (TGF-beta) is a member of a large family of pleiotropic cytokines that are involved in many biological processes, including growth control, differentiation, migration, cell survival, adhesion, and specification of developmental fate, in both normal and diseased states. TGF-beta superfamily members signal through a receptor complex comprising a type II and type I receptor, both serine/threonine kinases.

The type I receptors, referred to as activin receptor-like kinases (ALK), lie at the epicenter of the signaling cascade as they transduce TGF-beta signals to intracellular regulators of transcription known as Smad proteins. ALKs possess an extracellular binding domain, a transmembrane domain, a GS domain that serves as the site of activation by type II receptors, and a kinase domain that activates downstream 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. Some ALKs have been implicated in several disorders, including tumorigenesis and immune diseases, suggesting that these receptors can be used as drug targets.

Products Related to TGF-β Receptor(62)

  • GC11545 structure
    GC11545SB 431542
    CAS: 301836-41-9
    Purity: >98.00%

    SB 431542 is a highly potent and selective ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor, with an IC 50 value of 94nM.

  • GC10166 structure
    GC10166A 83-01
    CAS: 909910-43-6
    Purity: >98.00%

    A 83-01 is a potent and selective small-molecule inhibitor of TGF-β type I receptors ALK5, ALK4, and ALK7 (IC 50 =12nM, 45nM, 7.5nM).

  • GC10421 structure
    GC10421SB-505124 hydrochloride
    CAS: 356559-13-2
    Purity: >98%

    SB505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC 50 values of 129nM and 47nM for ALK4, ALK5, respectively.

  • GC11604 structure
    GC11604LY364947
    CAS: 396129-53-6
    Purity: >99.00%

    LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC 50 of 59nM.

  • GC11878 structure
    GC11878GW788388
    CAS: 452342-67-5
    Purity: >99.50%

    GW788388 is a potent and selective ALK5 inhibitor (IC₅₀=18nM). GW788388 also inhibits TGF-β type II receptor (IC₅₀=93nM) and activin type II receptor activity, but does not inhibit BMP type II receptors.

  • GC12108 structure
    GC12108ITD 1
    CAS: 1099644-42-4
    Purity: >99.50%

    ITD 1 is a selective TGFβ receptor inhibitor (IC 50 = 460nM).

  • GC12363 structure
    GC12363LY2109761
    CAS: 700874-71-1
    Purity: >99.50%

    LY2109761 is an orally available, small-molecule dual TGF-β receptor (TβR) I/II kinase inhibitor (TβRI: K i = 38nM; TβRII: K i = 300nM).

  • GC12560 structure
    GC12560Dorsomorphin (Compound C) 2HCl
    CAS: 1219168-18-9
    Purity: >98.00%

    Dorsomorphin (Compound C) 2HCl is a potent, cell-permeable dual inhibitor of AMPK and BMP pathways (K i value of 109nM for AMPK).

  • GC13225 structure
    GC13225LDN-214117
    CAS: 1627503-67-6
    Purity: >99.50%

    potent and selective ALK2 inhibitor

  • GC13354 structure
    GC13354EW-7197
    CAS: 1352608-82-2
    Purity: >99.00%

    EW-7197 is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5) with IC 50 value of 12.9nM.

  • GC13769 structure
    GC13769SB505124
    CAS: 694433-59-5
    Purity: >99.50%

    SB505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC 50 values of 129nM and 47nM for ALK4, ALK5, respectively.

  • GC13904 structure
    GC13904SD-208
    CAS: 627536-09-8
    Purity: >99.00%

    A potent, selective inhibitor of TGF-βRI

  • GC13927 structure
    GC13927A 77-01
    CAS: 607737-87-1
    Purity: >99.50%

    A potent ALK5 inhibitor

  • GC14298 structure
    GC14298DMH-1
    CAS: 1206711-16-1
    Purity: >99.00%

    DMH-1 is a selective bone morphogenetic protein (BMP) type I receptor ALK2 inhibitor with an IC 50 value of 108nM.

  • GC14349 structure
    GC14349SB525334
    CAS: 356559-20-1
    Purity: >98.00%

    SB525334 has been characterized as a potent and selective inhibitor of the transforming growth factor-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). SB525334 inhibited ALK5 kinase activity with an IC 50 of 14.3nM.

  • GC15567 structure
    GC15567K02288
    CAS: 1431985-92-0
    Purity: >98.00%

    ALK inhibitor

  • GC15892 structure
    GC15892Cetrimonium Bromide (CTAB)
    CAS: 57-09-0
    Purity: >98.00%

    Cetrimonium Bromide (CTAB), a common used surfactant, act as a drug solubilizer with intrinsic antibacterial properties.

  • GC16580 structure
    GC16580LDN-193189
    CAS: 1062368-24-4
    Purity: >99.00%

    ALK inhibitor,potent and selective

  • GC16793 structure
    GC16793RepSox
    CAS: 446859-33-2
    Purity: >98.00%

    RepSox is a potent and selective inhibitor of transforming growth factor-β receptor I/activin-like kinase 5 (TGF-β-RI/ALK5) with an IC 50 of 23nM. RepSox inhibits ALK5 autophosphorylation with an IC 50 of 4nM.

  • GC17035 structure
    GC17035LDN-212854
    CAS: 1432597-26-6
    Purity: >98.00%

    BMP receptor inhibitor,potent and selective

  • GC17243 structure
    GC17243Dorsomorphin (Compound C)
    CAS: 866405-64-3
    Purity: >98.00%

    Dorsomorphin (Compound C) is an agent that used as a cell-permeable AMPK inhibitor.

  • GC17582 structure
    GC17582ML347
    CAS: 1062368-49-3
    Purity: >98.00%

    BMP receptor inhibitor,potent and selective

  • GC18015 structure
    GC18015LY2157299
    CAS: 700874-72-2
    Purity: >98.00%

    LY2157299 is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC 50 value of 56nM.

  • GC19234 structure
    GC19234LY3200882
    CAS: 1898283-02-7
    Purity: >99.50%

    LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).