TGFßR1 (ALK5) Assay Service
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Target
TGFßR1 (ALK5)
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Description
Screening and/or profiling inhibitor compounds against TGFBR1 serine-threonine kinase activity in a biochemical assay.
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Synonyms
TGFBR1, ALK5, SKR4, TGF-beta receptor type-1, TGFR-1, Activin A receptor type II-like protein kinase of 53kD, Activin receptor-like kinase 5 (ALK-5; ALK5), Serine/threonine-protein kinase receptor R4 (SKR4), TGF-beta type I receptor
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Example Data
*Example only, final data may vary.
Assay Details
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Assay Format
Luminescent
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Reference Compounds and IC50
A83-01, 7 nM
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Assay Principle
The transforming growth factor beta receptor (TGFβR1, also known as ALK5) Kinase Assay is designed to measure the serine/threonine activity of TGFβR1 (ALK5) for screening and profiling applications using ADP-Glo® as a detection reagent that measures ATP formed from ADP using light generated in a luciferase reaction.
Target Details
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Protein Family
Kinases
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UniProt
P36897
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Background
The transforming growth factor beta (TGFB) signaling pathway regulates a wide range of biological and cellular processes including cell growth, differentiation, survival/apoptosis, and migration. TGFβ binds to a type II receptor dimer, which recruits a type I receptor dimer forming a hetero-tetrameric complex. The TGFβ receptor is a transmembrane serine/threonine kinase that phosphorylates proteins of the SMAD (Mothers against decapentaplegic homolog) family. Due to its role in immunosuppression, cancer, and inflammatory diseases, among others, this receptor is an attractive therapeutic target.
Delivery
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Estimated Turnaround
Two to three weeks following delivery of compounds
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Results
Extensive report with raw and analyzed data, graphs, and detailed protocols. Includes positive control for inhibition.
