In Vitro Efficacy Testing Services for Scleroderma

We provide robust and sensitive in vitro screening and characterization platforms for accelerating the discovery and screening of potential therapies for Scleroderma. Our services enable the evaluation of candidate compounds targeting key fibrotic and immune-mediated pathways implicated in Scleroderma, such as TGF-β signaling, collagen synthesis, and inflammatory cytokine activity. By utilizing disease-relevant cellular and molecular assays, we assess effects on fibroblast activation, extracellular matrix production, and immune cell function. These approaches allow for detailed investigation of pathological processes including fibrosis, immune dysregulation, and tissue remodeling.

Our testing portfolio encompasses a comprehensive range of biochemical and cell-based assays designed to evaluate therapeutic efficacy, mechanism of action, and target engagement. We offer advanced detection technologies including fluorescence, luminescence, and mass spectrometry, enabling precise measurement of molecular interactions, enzymatic activity, and cellular responses. These methods support high-throughput screening and in-depth pharmacological profiling for Scleroderma research.

Bioluminescence resonance energy transfer (BRET) assay: Measures protein-protein interactions and receptor activity in real time, providing insights into intracellular signaling relevant to Scleroderma.

Cell counting assay: Quantifies cell proliferation and viability, useful for assessing antiproliferative or cytotoxic effects of test compounds on fibrotic or immune cell populations.

Chemiluminescent assay: Detects specific analytes or enzymatic activities with high sensitivity, supporting quantification of biomarkers involved in fibrosis or inflammation.

ELISA assay: Enables quantification of proteins, cytokines, or other soluble factors involved in Scleroderma pathogenesis, such as TGF-β or collagen.

FS-3 as substrate: Utilized in enzymatic assays to measure protease activity, relevant for studying matrix remodeling enzymes in Scleroderma.

Flow cytometry assay: Offers multiparametric analysis of cell surface markers and intracellular molecules, facilitating characterization of immune cell subsets and activation states.

Fluorescence resonance energy transfer (FRET) assay: Detects molecular interactions and conformational changes, aiding in the study of signaling events relevant to fibrosis.

Fluorescent assay: Broadly applicable for measuring cellular events, enzyme activities, or reporter gene expression using fluorescent readouts.

Fluorescent polarization assay: Assesses binding interactions between small molecules and target proteins, supporting the identification of therapeutic candidates.

Homogeneous Time Resolved Fluorescence (HTRF) assay: Delivers sensitive quantification of biomolecular interactions or analytes involved in Scleroderma pathology.

Mass spectrometry: Provides precise identification and quantification of proteins, metabolites, or signaling molecules, enabling comprehensive pathway analysis.

Microfluidic mobility shift assay: Measures changes in molecular size or charge, useful for enzyme activity studies and inhibitor screening.

Occupancy assay: Determines the extent of target engagement by compounds, supporting mechanism-of-action studies.

RNA assay: Quantifies gene expression changes in response to treatment, helping to elucidate molecular effects on fibrotic or immune pathways.

Surface plasmon resonance assay: Analyzes real-time binding kinetics between molecules, supporting the characterization of drug-target interactions.

Surface plasmon resonance assay (+ATP): Assesses binding interactions in the presence of ATP, relevant for kinases or ATP-dependent processes.

We measure a range of pharmacological parameters to assess compound potency, efficacy, and selectivity. These include concentration-response metrics, binding affinities, and minimal effective concentrations, providing critical data for lead optimization and preclinical evaluation. Accurate parameter determination ensures effective candidate selection and guides subsequent drug development decisions.

EC-50: The concentration of a drug that produces 50% of its maximal effect, indicating compound potency.

IC-50: The concentration required to inhibit a biological process or target by 50%, widely used to compare inhibitor efficacy.

Kd: The equilibrium dissociation constant, reflecting the binding affinity between a drug and its target; lower values indicate stronger binding.

MEC: Minimum effective concentration, the lowest concentration at which a drug elicits a measurable biological response.

MED: Minimum effective dose, the smallest dose that produces a desired therapeutic effect, important for determining dosing regimens.

MIC: Minimum inhibitory concentration, the lowest concentration of a compound that prevents a defined biological or microbial activity; used for antimicrobial and cytostatic evaluations.

Recommended In Vitro Efficacy Tests

Bruton Tyrosine Kinase

Bruton Tyrosine Kinase (BTK) plays a key role in Scleroderma by mediating immune cell signaling and fibrosis. BTK testing is critical for evaluating drug efficacy and safety in Scleroderma therapies. Our service offers BTK occupancy, flow cytometry, chemiluminescent, and microfluidic mobility shift assays to assess drug-target engagement. Main parameters measured include IC-50 (half-maximal inhibitory concentration) and MED (minimum effective dose), supporting precise dose selection in drug development.

Cereblon

Cereblon, a key E3 ubiquitin ligase, mediates the therapeutic and adverse effects of certain Scleroderma drugs. Accurate Cereblon testing is essential for optimizing drug efficacy and safety. Our service utilizes FRET, chemiluminescent, BRET, HTRF, and fluorescent polarization assays to assess compound binding and activity. We provide critical pharmacological parameters including EC-50, IC-50, and Kd, supporting informed decision-making in Scleroderma drug development.

Ectonucleotide Pyrophosphatase/Phosphodiesterase 2

Ectonucleotide Pyrophosphatase/Phosphodiesterase 2 (ENPP2) is implicated in Scleroderma pathogenesis by regulating lysophospholipid signaling and fibrosis. ENPP2 testing is crucial for identifying inhibitors and optimizing drug candidates. Our service employs FS-3 substrate-based fluorescent assays and mass spectrometry to accurately quantify ENPP2 activity, determining IC50 values for potential therapeutics. This enables precise evaluation of drug efficacy in modulating ENPP2 for Scleroderma treatment development.

Endothelin Receptor Type A

Endothelin Receptor Type A (ETA) mediates vasoconstriction and fibrosis in Scleroderma pathogenesis. ETA testing is crucial for evaluating drug candidates targeting fibrotic and vascular complications. Key methods include radioligand binding assays, cell-based functional assays, and gene/protein expression analysis. Main parameters measured are receptor binding affinity, functional inhibition (IC50), and downstream signaling activity, providing critical data for Scleroderma drug development.

Glutamyl-Prolyl-Trna Synthetase 1

Glutamyl-Prolyl-Trna Synthetase 1 is implicated in Scleroderma pathogenesis through its role in protein synthesis and immune modulation. Our testing service employs surface plasmon resonance assays (with and without ATP) to characterize ligand binding to this enzyme. Determining the dissociation constant (Kd) enables precise evaluation of drug candidates targeting Glutamyl-Prolyl-Trna Synthetase 1, supporting rational Scleroderma drug development and therapeutic optimization.

Il2 Inducible T Cell Kinase

Our Il2 Inducible T Cell Kinase (ITK) testing service supports Scleroderma drug development by assessing ITK’s role in T cell signaling, a key driver of disease pathology. This service employs occupancy assays, microfluidic mobility shift assays, and ELISA to evaluate compound efficacy. Key parameters measured include IC-50 (half-maximal inhibitory concentration) and MED (minimum effective dose), providing critical data for candidate selection and optimization.

Tumor Necrosis Factor

Tumor Necrosis Factor (TNF) plays a pivotal role in Scleroderma pathogenesis by driving inflammation and fibrosis. TNF testing is crucial for Scleroderma drug development to evaluate anti-inflammatory efficacy. Our service employs cell counting assays, chemiluminescent assays, and RNA assays to assess drug impact on TNF activity. Key parameters measured include EC-50, MEC, and MIC, providing precise insights into compound potency and therapeutic potential.