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Activin A Inhibitors

" in MedChemExpress (MCE) Product Catalog:

29

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生化学アッセイ試薬

4

阻害性抗体

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同位体標識化合物

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製品番号 製品名 Target 研究分野 構造式
  • HY-13012
    RepSox
    Maximum Cited Publications
    21 Publications Verification

    E-616452; SJN 2511

    		 Organoid TGF-β Receptor Metabolic Disease
    RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes .
    RepSox
  • HY-19928
    Vactosertib
    5+ Cited Publications

    EW-7197; TEW-7197

    		 TGF-β Receptor Cancer
    Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect .
    Vactosertib
  • HY-P99632
    Garetosmab
    1 Publications Verification

    REGN 2477

    		 TGF-β Receptor Inflammation/Immunology
    Garetosmab (REGN 2477) is a fully human IgG4 monoclonal antibody that specifically inhibits activin A. Garetosmab can be used for fibrodysplasia ossificans progressiva (FOP) research .
    Garetosmab
  • HY-P99590A
    Sotatercept (mIgG2a)
    1 Publications Verification

    RAP-011

    		 TGF-β Receptor TGF-beta/Smad Cardiovascular Disease Metabolic Disease
    Sotatercept (mIgG2a) (RAP-011), the murine homolog of Sotatercept (ACE-011) (HY-P99590), is a soluble activin receptor type IIA (ActRIIA) ligand trap. Sotatercept (mIgG2a) inhibits the binding of activin A and other members of the TGF-β superfamily (such as Activin A/B, GDF11 and BMP9/10) to their receptors by combining and neutralizing them, thereby regulating cell proliferation and differentiation. Sotatercept (mIgG2a) mainly inhibits the SMAD2/3 signaling pathway, and can be used in various diseases such as chronic kidney disease. Sotatercept (mIgG2a) reduces the expression of erythropoietic hepcidin (ERFE), regulates iron metabolism, and promotes red blood cell production. Sotatercept (mIgG2a) has a dual effect of promoting bone formation (anabolic) and inhibiting bone resorption (catabolic) .
    Sotatercept (mIgG2a)
  • HY-10326
    GW788388
    15+ Cited Publications

    		 TGF-β Receptor Cancer
    GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
    GW788388
  • HY-19928A
    Vactosertib Hydrochloride
    5+ Cited Publications

    EW-7197 Hydrochloride; TEW-7197 Hydrochloride

    		 TGF-β Receptor Cancer
    Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect .
    Vactosertib Hydrochloride
  • HY-78349
    A 77-01
    2 Publications Verification

    		 TGF-β Receptor Cancer
    A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM .
    A 77-01
  • HY-117887
    Fidrisertib

    BLU-782; IPN-60130; ALK2-IN-1

    		 TGF-β Receptor Cancer
    Fidrisertib (BLU-782) is the orally active inhibitor for activin receptor-like kinase 2 (ALK2) that inhibits ALK2 R206H, ALK2, ALK1, ALK6, ALK3, ALK4, TGFβR2 and ALK5 with IC50s of 0.2, 0.6, 3, 24, 45, 65, 67 and 155 nM, respectively .
    Fidrisertib
  • HY-136773
    KER047

    ALK2-IN-4

    		 TGF-β Receptor Metabolic Disease
    KER047 (ALK2-IN-4) is a potent activin receptor-like kinase-2 (ALK2) inhibitor. KER047 can be used for the research of metabolic disease, such as fibrodysplasia ossificans progressiva (FOP).
    KER047
  • HY-P99818
    Ramatercept

    ACE-031

    		 TGF-β Receptor Metabolic Disease
    Ramatercept (ACE-031) is a soluble ActRIIB receptor and can be used as a soluble activin receptor 2 (ACVR2) antagonist. Ramatercept inhibits the signal pathway of muscle growth inhibition and has potential application in muscle atrophy .
    Ramatercept
  • HY-151289
    ALK5-IN-34

    		TGF-β Receptor TGF-beta/Smad Cancer
    ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .
    ALK5-IN-34
  • HY-125851
    TP-008

    		TGF-β Receptor Inflammation/Immunology
    TP-008, a chemical probe, is a potent, selective and orally active (Activin-Like Kinase 5) ALK5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose .
    TP-008
  • HY-173149
    CDD-2789

    		Anaplastic lymphoma kinase (ALK) TGF-beta/Smad TGF-β Receptor Cancer
    CDD-2789 is a potent and selective ALK2 inhibitor with an IC50 0.54 μM and a Kd of 2.1 nM, respectively. CDD-2789 exhibits >120-fold selectivity over ALK3/5/6. CDD-2789 reduces activin A- and BMP2-induced SMAD1/5 phosphorylation in fibroblasts. CDD-2789 can be used for ALK2-related cancer research .
    CDD-2789
  • HY-155939
    M4K2163 dihydrochloride

    		TGF-β Receptor Cancer
    M4K2163 dihydrochloride is a potent, selective, blood-brain barrier (BBB) permeable activin receptor-like kinase-2 (ALK2) inhibitor, with an IC50 of 19 nM. M4K2163 dihydrochloride can be used in the research of diffuse intrinsic pontine glioma (DIPG) .
    M4K2163 dihydrochloride
  • HY-P990720
    Elritercept

    KER-050

    		 TGF-beta/Smad Inflammation/Immunology
    Elritercept (KER-050) is a recombinant fusion protein comprising a modified activin receptor type IIA extracellular domain fused to a human IgG1 Fc. Elritercept inhibits activin A and other select TGF-β superfamily ligands .
    Elritercept
  • HY-13012R
    RepSox (Standard)

    E-616452 (Standard); SJN 2511 (Standard)

    		 Organoid TGF-β Receptor Reference Standards Metabolic Disease
    RepSox (Standard) is the analytical standard of RepSox. This product is intended for research and analytical applications. RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes .
    RepSox (Standard)
  • HY-122179
    NUCC-555

    		TGF-β Receptor Inflammation/Immunology
    NUCC-555 is an activin antagonist. NUCC-555 interacts with Trp25, Trp28, Phe55, Tyr93, Lys103, and Asn107 in the Activin A binding pocket. NUCC-555 blocks Activin A-mediated hepatic stellate cells (HSCs) activation. NUCC-555 promotes liver regeneration and halts fibrosis progression in chronic liver disease models. NUCC-555 inhibits Activin A-mediated ovarian cell proliferation. NUCC-555 decreases FSH levels in ovariectomized mice .
    NUCC-555
  • HY-149403
    J-1048

    		Anaplastic lymphoma kinase (ALK) Others
    J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor. J-1048 can inhibit TAA-induced liver fibrosis in mice by explicitly blocking the TGF-β/Smad signaling pathway .
    J-1048
  • HY-161377
    M4K2306

    		TGF-β Receptor Cancer
    M4K2306 is a selective inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 7 nM. M4K2306 is blood brain permeable with a brain to plasma ratio of 75.6 .
    M4K2306
  • HY-151272
    ALK5-IN-26

    		Anaplastic lymphoma kinase (ALK) Cancer
    ALK5-IN-26 (EX-22) is an ALK (Activin receptor-like kinase) inhibitor. ALK5-IN-26 inhibits ALK5 with an IC50 value ≤10 nM. ALK5-IN-26 can be used for the research of cancer .
    ALK5-IN-26
  • HY-136773A
    KER047 succinate

    ALK2-IN-4 succinate

    		 TGF-β Receptor Metabolic Disease
    KER047 succinate (ALK2-IN-4 succinate) is a potent activin receptor-like kinase-2 (ALK2) inhibitor. KER047 succinate can be used for the research of metabolic disease, such as fibrodysplasia ossificans progressiva (FOP).
    KER047 succinate
  • HY-161376
    M4K2281

    		TGF-β Receptor Cancer
    M4K2281 is a selecitve inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 2 nM. M4K2281 exhibits a moderate blood brain permeability with a brain to plasma ratio of 3.7 at 4h .
    M4K2281
  • HY-W707119
    RepSox hydrochloride

    E-616452 hydrochloride; SJN 2511 hydrochloride

    		 TGF-beta/Smad Anaplastic lymphoma kinase (ALK) Metabolic Disease
    RepSox hydrochloride is a potent and selective inhibitor of transforming growth factor-β receptor I/activin-like kinase 5 (TGF-β-RI/ALK5). RepSox hydrochloride inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox hydrochloride can be used in the study of obesity and related metabolic diseases such as type 2 diabetes.
    RepSox hydrochloride
  • HY-151277
    ALK5-IN-29

    		Anaplastic lymphoma kinase (ALK) Cancer
    ALK5-IN-29 is an selective activin receptor-like kinase (ALK) inhibitor. ALK5-IN-29 can inhibit the activity of ALK5 with an IC50 value of ≤10 nM. ALK5-IN-29 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .
    ALK5-IN-29
  • HY-162902
    ALK5-IN-82

    		TGF-β Receptor Cardiovascular Disease
    ALK5-IN-82 is a potent and selective inhibitor against activin receptor-like kinase 5 (ALK5) with an IC50 value of 9.1 nM. ALK5-IN-82 inhibits the protein expression of α-smooth muscle actin (α-SMA), collagen I and tissue inhibitor of metalloproteinase 1 (TIMP-1)/matrix metalloproteinase 13 (MMP-13) in transforming growth factor-β-induced human umbilical vein endothelial cells. ALK5-IN-82 is promising for research of cardiac fibrosis .
    ALK5-IN-82
  • HY-10326R
    GW788388 (Standard)

    		Reference Standards TGF-β Receptor Cancer
    GW788388 (Standard) is the analytical standard of GW788388 (HY-10326). This product is intended for research and analytical applications. GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
    GW788388 (Standard)
  • HY-183005
    ActRIIB-IN-1

    		TGF-β Receptor Inflammation/Immunology Cancer
    ActRIIB-IN-1, 7-azaindole compound is an orally active activin type II receptor B (ActRIIB) inhibitor with an IC50 of 1.8 nM. ActRIIB-IN-1 can alleviate weight loss, muscle atrophy and decreased muscle strength caused by tumor cachexia, as well as improve appetite. ActRIIB-IN-1 can be used for the research of cancer cachexia .
    ActRIIB-IN-1
  • HY-13012S
    RepSox-d5

    E-616452-d5; SJN 2511-d5

    		 Isotope-Labeled Compounds TGF-β Receptor Metabolic Disease
    RepSox-d5 (E-616452-d5) is the deuterium labeled RepSox (HY-13012). RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes .
    RepSox-d5
  • HY-10321G
    PD173074

    		FGFR TGF-beta/Smad Cancer
    PD173074 GMP is PD173074 (HY-10321) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. PD173074 is an orally active FGFR inhibitor that targets the transphosphorylation of FGFR1 and FGFR2 and blocks the FGF signaling pathway. By reducing the phosphorylation level of SMAD2 and altering the expression of Nodal/Activin target genes, PD173074 eliminates endothelial differentiation potential, thereby inhibiting the formation of capillary-like structures. PD173074 blocks the proliferation and colony formation of tumor cells and increases intratumoral cell apoptosis. PD173074 successfully reverses FGF-2-induced chemoresistance to enhance the effect of cisplatin (HY-17394) in small cell lung cancer models. PD173074 can be applied to research related to critical limb ischemia and small cell lung cancer .
    PD173074

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