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Applications: Study and screen compounds that inhibit the binding of Activin A to Activin RIIB for drug discovery in high throughput screening (HTS) applications.
Background: Activin A is a member of the TGFβ (transforming growth factor beta) family of proteins involved in embryonic development, hematopoiesis, cell proliferation, and cell differentiation. It is the ligand to the activin A receptor type I or type II, which are transmembrane receptors with serine/threonine kinase activity. Upon binding of activin, the kinase activity of the receptor is activated, SMAD2 (mothers against decapentaplegic homolog 2) and SMAD3 are phosphorylated, form a complex with SMAD4 and translocate to the nucleus, regulating gene expression. Activin A can be found in macrophages, dendritic cells, and neutrophils, playing a role in cell maturation and activation. It is involved in inflammation and autoimmune disorders, such as SLE (systemic lupus erythematosus), RA (rheumatoid arthritis), and atopic dermatitis. It is also involved in bone formation. The use of fusion protein blockers of the activin signaling pathways, that serve as sinks for activin A and other TGFβ members, is being explored for the treatment of pulmonary hypertension, chemotherapy-induced anemia, and osteoporosis.
Contraindications: The Activin A:Activin RIIB Binding Assay Kit is compatible with up to 1% final DMSO concentration.
Description: The Activin A: Activin RIIB [Biotinylated] Inhibitor Screening Assay Kit is an ELISA-based assay designed to measure the binding between Activin A and Activin RIIB (receptor IIB), also known as ACVR2B, protein for screening and profiling applications. This kit comes with enough purified Activin A (amino acids 311-426) and biotinylated Activin Receptor IIB (amino acids 19-137), streptavidin-HRP, assay buffer, and detection reagent for 100 enzyme reactions.A 96-well plate is coated with Activin A protein. After coating and blocking, biotinylated Activin RIIB, also known as ACVR2B, is added in an optimized assay buffer. Next, unbound biotinylated Activin RIIB is washed away, and the plate is incubated with streptavidin-HRP. After a final wash, ELISA ECL substrate is added to produce chemiluminescence that can be measured using a chemiluminescence reader. The chemiluminescence signal is proportional to the efficacy of Activin RIIB binding to Activin A.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Uniprot: P36896
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Lodberg A., 2021 Cytokine & Growth Factor Reviews 60:1-17.
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