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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 .
Sotatercept (ACE-011) is a soluble activin receptor 2A (ACVR2A) type IgG Fc fusion protein. Sotatercept combines activin and growth differentiation factor to try to restore the balance between growth promotion and growth inhibition signal pathways. Sotatercept has potential application in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, multiple myeloma (MM) osteolytic lesions .
ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3 .
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.
Ramatercept 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 .
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 .
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 .
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 .
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 .
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) .
TP-008 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 .
Bimagrumab (Anti-ACVR2B Reference Antibody) is a human monoclonal antibody that blocks activin type II receptor (ActRII), with KDs of 1.7 pM and 434 pM for human ActRIIB and ActRIIA, respectively. Bimagrumab can be used for the research of pathological muscle loss and weakness .
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 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 .
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 .
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 .
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 .
The transforming growth factor beta (TGF-β) signaling pathway is involved in many cellular processes in both the adult organism and the developing embryo including cell growth, cell differentiation, apoptosis, cellular homeostasis and other cellular functions. The TGF-β superfamily comprises TGF-βs, bone morphogenetic proteins (BMPs), activins and related proteins. Signaling begins with the binding of a TGF beta superfamily ligand to a TGF beta type II receptor. The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the Type I receptor. The type I receptor then phosphorylates receptor-regulated SMADs (R-SMADs) which can now bind the coSMAD (e.g. SMAD4). R-SMAD/coSMAD complexes accumulate in the nucleus where they act as transcription factors and participate in the regulation of target gene expression. Deregulation of TGF-β signaling contributes to developmental defects and human diseases, including cancers, some bone diseases, chronic kidney disease, etc.
MCE designs a unique collection of 223 TGF-beta/Smad signaling pathway compounds. TGF-beta/Smad Compound Library acts as a useful tool for TGF-beta/Smad-related drug screening and disease research.
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 .
Sotatercept (ACE-011) is a soluble activin receptor 2A (ACVR2A) type IgG Fc fusion protein. Sotatercept combines activin and growth differentiation factor to try to restore the balance between growth promotion and growth inhibition signal pathways. Sotatercept has potential application in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, multiple myeloma (MM) osteolytic lesions .
Bimagrumab (Anti-ACVR2B Reference Antibody) is a human monoclonal antibody that blocks activin type II receptor (ActRII), with KDs of 1.7 pM and 434 pM for human ActRIIB and ActRIIA, respectively. Bimagrumab can be used for the research of pathological muscle loss and weakness .
Ramatercept 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 .
Prafnosbart (DS-6016A) is an IgG1-kappa, anti-ACVR1 (activin A receptor type 1, ACVRLK2, ALK2, ACVR1A, SKR1) humanized monoclonal antibody. Prafnosbart can be used for bone metabolism disorders research .
The INHBA protein plays a key role in regulating pituitary function by regulating follicle-stimulating hormone secretion together with activin. Its broad effects span a variety of physiological processes, including hormone secretion, germ cell development, erythrocyte differentiation, insulin secretion, nerve cell survival, embryonic development, and bone growth, depending on unique subunit composition. GMP Activin A Protein, Human/Mouse/Rat (HEK293) is the recombinant rat, mouse, human-derived Activin A protein, expressed by HEK293 , with tag free. The total length of GMP Activin A Protein, Human/Mouse/Rat (HEK293) is 116 a.a., with molecular weight of 13-15 kDa.
Activin A, a multifunctional cytokine, is a member of TGF-β superfamily. Activin A first binds to the type II activin receptors (ActIIRA or ActRIIB) on the member surface, and then recruits and phosphorylates type I activin receptors (ActRI). Activin A primarily signal through SMAD2/3 proteins to regulate a variety of functions, including inflammation, fibrosis, and tumorigenesis. Activin A Protein, Human/Mouse/Rat (HEK293) is produced in HEK293 cells, and consists of 117 amino acids (G310-S426).
Activin A, a multifunctional cytokine, is a member of TGF-β superfamily. Activin A first binds to the type II activin receptors (ActIIRA or ActRIIB) on the member surface, and then recruits and phosphorylates type I activin receptors (ActRI). Activin A primarily signal through SMAD2/3 proteins to regulate a variety of functions, including inflammation, fibrosis, and tumorigenesis. Activin A Protein, Mouse (HEK293, His) is produced in HEK293 cellswith a C-Terminal His-tag. It consists of 424 amino acids (M1-S424).
Activin A, a multifunctional cytokine, is a member of TGF-β superfamily. Activin A first binds to the type II activin receptors (ActIIRA or ActRIIB) on the member surface, and then recruits and phosphorylates type I activin receptors (ActRI). Activin A primarily signal through SMAD2/3 proteins to regulate a variety of functions, including inflammation, fibrosis, and tumorigenesis. Activin A Protein, Mouse (HEK293, His) is produced in HEK293 cellswith a C-Terminal His-tag. It consists of 404 amino acids (S21-S424).
ACVR2A, also known as Activin RIIA, is an activin type II receptor. On ligand binding, ACVR2A can forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. ACVR2A is a receptor for Activin A, Activin B and Inhibin A. ACVR2A/Activin RIIA Protein, Human (HEK293, Fc) is produced in HEK293 cells with a C-Terminal Fc-tag. It consists of 134 amino acids (M1-P134).
ACVR2A, also known as Activin RIIA, is an activin type II receptor. On ligand binding, ACVR2A can forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. ACVR2A is a receptor for Activin A, Activin B and Inhibin A. ACVR2A/Activin RIIA Protein, Mouse (HEK293, His) is produced in HEK293 cells with a C-Terminal His-tag. It consists of 134 amino acids (M1-P134).
ACVR2A, also known as Activin RIIA, is an activin type II receptor. On ligand binding, ACVR2A can forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. ACVR2A is a receptor for Activin A, Activin B and Inhibin A. ACVR2A/Activin RIIA Protein, Mouse (HEK293, His-Fc) is produced in HEK293 cells with a C-Terminal His-tag and a C-Terminal Fc-tag. It consists of 134 amino acids (M1-P134).
ACVR2A, also known as Activin RIIA, is an activin type II receptor. On ligand binding, ACVR2A can forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. ACVR2A is a receptor for Activin A, Activin B and Inhibin A. ACVR2A/Activin RIIA Protein, Human (HEK293, His) is produced in HEK293 cells with six C-Terminal His-tags. It consists of 115 amino acids (A20-P134).
ACVR2A, also known as Activin RIIA, is an activin type II receptor. On ligand binding, ACVR2A can forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. ACVR2A is a receptor for Activin A, Activin B and Inhibin A. ACVR2A/Activin RIIA Protein, Human (HEK293, His) is produced in HEK293 cells with six C-Terminal His-tags. It consists of 115 amino acids (A20-P134).
The INHBA protein plays a key role in regulating pituitary function by regulating follicle-stimulating hormone secretion together with activin. Its broad effects span a variety of physiological processes, including hormone secretion, germ cell development, erythrocyte differentiation, insulin secretion, nerve cell survival, embryonic development, and bone growth, depending on unique subunit composition. Animal-Free Activin A Protein, Human/Mouse/Rat (His) is the recombinant human, rat, mouse-derived animal-FreeActivin A protein, expressed by E. coli , with C-His labeled tag. The total length of Animal-Free Activin A Protein, Human/Mouse/Rat (His) is 116 a.a., with molecular weight of ~13.9 kDa.
Activin A receptor, type I (ACVR1), also known as ALK-2, is a bone morphogenetic protein (BMP) type I receptor. ACVR1 is involved in a wide variety of biological processes, including bone, heart, cartilage, nervous, and reproductive system development and regulation. Activin RIA Protein, Human (HEK293, Fc) is produced in HEK293 cells with a C-Terminal Fc-tag. It consists of 102 amino acids (D23-V124).
