In Vitro Efficacy Testing Services for Lupus Erythematosus
Drug R&D Solutions

In Vitro Efficacy Testing Services for Lupus Erythematosus

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We provide robust and sensitive in vitro screening and characterization platforms for accelerating the discovery and screening of potential therapies for Lupus Erythematosus. Our services enable comprehensive evaluation of drug candidates targeting autoimmune responses, inflammation, and immune cell signaling relevant to Lupus. Key targets include cytokines (e.g., IFN-α, TNF-α), autoantibodies, complement proteins, and pathways such as JAK/STAT and NF-κB. We can assess cellular activation, cytokine production, and autoantibody generation, supporting the understanding and modulation of pathological immune mechanisms involved in Lupus.

We offer a broad spectrum of in vitro testing methods, including biochemical, cell-based, and biophysical assays, tailored to evaluate efficacy and mechanism of action for Lupus drug candidates. These methods enable sensitive measurement of target engagement, functional activity, and molecular interactions essential in autoimmune disease research.

ATP assay: Measures cellular ATP levels as an indicator of cell viability or cytotoxicity, providing insights into the effects of compounds on immune cell metabolism.

Bioluminescence resonance energy transfer (BRET) assay: Detects molecular interactions in live cells, useful for studying protein-protein interactions relevant to Lupus signaling pathways.

Chemiluminescent assay: Quantifies biological molecules using light emission, enabling sensitive detection of cytokines, autoantibodies, or complement components.

ELISA assay: A high-throughput immunoassay for quantifying proteins such as cytokines, autoantibodies, and biomarkers in cell supernatants or serum.

Fluorescence resonance energy transfer (FRET) assay: Monitors biomolecular interactions or enzymatic activities, supporting analysis of signaling cascades implicated in Lupus.

Fluorescent assay: General fluorescence-based assays to measure cell function, binding events, or enzymatic activity in immune and inflammatory processes.

Fluorescent polarization assay: Assesses binding interactions by detecting changes in fluorescence polarization, ideal for characterizing immune complex formation.

Homogeneous Time Resolved Fluorescence (HTRF) assay: Combines FRET and time-resolved measurements for sensitive, homogeneous detection of molecular interactions or analytes.

Luciferine/luciferase assay: Utilizes luciferase enzyme activity to report cellular events or gene expression changes linked to immune activation.

Mass spectrometry: Provides precise identification and quantification of proteins, peptides, or metabolites, facilitating biomarker discovery and pathway analysis.

Surface plasmon resonance assay: Real-time, label-free analysis of biomolecular binding kinetics, valuable for characterizing drug-target interactions and antibody binding.

Our assays measure critical pharmacological parameters such as IC-50, Kd, and MIC to evaluate compound potency, binding affinity, and antimicrobial activity. These quantitative metrics inform lead optimization and candidate selection by providing data on efficacy, specificity, and therapeutic potential.

IC-50: The concentration of a compound required to inhibit a specific biological process by 50%, a key metric for assessing drug potency.

Kd: The equilibrium dissociation constant indicating the affinity between a drug and its target; lower Kd values reflect stronger binding interactions essential for effective inhibition or modulation.

MIC: The minimum inhibitory concentration needed to prevent microbial or cellular growth, important for evaluating the efficacy of compounds in controlling pathogenic or immune-related processes.

Recommended In Vitro Efficacy Tests

Bruton Tyrosine Kinase

Bruton Tyrosine Kinase (BTK) is a key mediator in B-cell signaling, implicated in the pathogenesis of Lupus Erythematosus. BTK testing is vital for evaluating drug candidates targeting this pathway. Our service utilizes chemiluminescent, surface plasmon resonance, and FRET assays to assess inhibitor potency and binding. Critical parameters measured include IC-50 for inhibitory concentration and Kd for binding affinity, supporting robust drug development decisions.

Pharmacological Activity Material Method Parameter
Protein-tyrosine kinase (BTK) (C481S-mutated) affinity Recombinant human enzyme Surface plasmon resonance assay Kd
Protein-tyrosine kinase (BTK) (C481S-mutated) affinity IC-50
Protein-tyrosine kinase (BTK) (C481S-mutated), inhibition Recombinant human enzyme Fluorescence resonance energy transfer (FRET) assay IC-50
Protein-tyrosine kinase (BTK) (C481S-mutated), inhibition Chemiluminescent assay IC-50
Protein-tyrosine kinase (BTK) (L528W-mutated), inhibition IC-50
Protein-tyrosine kinase (BTK) (T474I-mutated) affinity Recombinant human enzyme Surface plasmon resonance assay Kd
Protein-tyrosine kinase (BTK) (T474I-mutated) affinity IC-50
Protein-tyrosine kinase (BTK) affinity Recombinant human enzyme Surface plasmon resonance assay Kd
Protein-tyrosine kinase (BTK) affinity IC-50
Protein-tyrosine kinase (BTK), inhibition Chemiluminescent assay IC-50

Caspase 1

Caspase 1 plays a pivotal role in Lupus Erythematosus by mediating inflammatory pathways and cytokine activation. Caspase 1 testing is crucial for evaluating drug efficacy targeting inflammation in lupus. Our service employs a sensitive chemiluminescent assay to quantify Caspase 1 activity, providing accurate measurement of the minimal inhibitory concentration (MIC) for drug candidates, thereby facilitating informed decisions in lupus drug development.

Pharmacological Activity Material Method Parameter
Caspase-1 (cleaved) expression, inhibition Müller glial cells (retinal), mouse (hypoxic) Chemiluminescent assay MIC

Cereblon

Cereblon is a key E3 ligase involved in the mechanism of immunomodulatory drugs for Lupus Erythematosus. Testing its activity is crucial for optimizing drug efficacy and safety. Our service utilizes BRET and HTRF assays to assess Cereblon-ligand interactions, providing quantitative IC-50 values to guide compound selection and development. This enables precise evaluation of drug candidates targeting Cereblon in Lupus therapy.

Pharmacological Activity Material Method Parameter
Cereblon affinity HEK293T human embryonic kidney cells transfected with protein/luciferase Bioluminescence resonance energy transfer (BRET) assay IC-50
Cereblon affinity Recombinant human enzyme Homogeneous Time Resolved Fluorescence (HTRF) assay IC-50
Cereblon affinity Homogeneous Time Resolved Fluorescence (HTRF) assay IC-50

Cyclic Gmp-Amp Synthase

Cyclic GMP-AMP Synthase (cGAS) is a key sensor in the innate immune response, implicated in the pathogenesis of Lupus Erythematosus via aberrant activation. Our cGAS testing service supports drug development by assessing compound efficacy using multiple methods, including luciferase, mass spectrometry, ATP, ELISA, fluorescent, chemiluminescent, and fluorescent polarization assays. The primary parameter measured is IC-50, enabling precise evaluation of cGAS inhibition potency for candidate therapeutics.

Pharmacological Activity Material Method Parameter
Cyclic GMP-AMP synthase (cGAS), inhibition Human enzyme ATP assay IC-50
Cyclic GMP-AMP synthase (cGAS), inhibition Human enzyme Fluorescent polarization assay IC-50
Cyclic GMP-AMP synthase (cGAS), inhibition Recombinant human enzyme Mass spectrometry IC-50
Gene (interferon-stimulated response element) transcription (dsDNA-induced), inhibition THP1 human acute monocytic leukemia cells transfected with IRF/luciferase (cGAMP-stimulated) Luciferine/luciferase assay IC-50
Gene (interferon-stimulated response element) transcription (dsDNA-induced), inhibition THP1 human acute monocytic leukemia cells transfected with double stranded DNA for cGAS/IRF/luciferase Luciferine/luciferase assay IC-50
Interferon alpha-2 production, inhibition Blood, human (double stranded DNA-stimulated) Chemiluminescent assay IC-50
Interferon beta production, inhibition THP1 human acute monocytic leukemia cells (phorbol ester-treated) ELISA assay IC-50
Interferon beta production, inhibition THP1 human acute monocytic leukemia cells (phorbol ester-treated) Fluorescent assay IC-50

Cyclin Dependent Kinase 7

Cyclin Dependent Kinase 7 (CDK7) regulates transcription and cell cycle progression, contributing to immune dysregulation in Lupus Erythematosus. Testing CDK7 inhibitors is crucial for identifying novel therapeutic candidates. Our service employs sensitive ATP assays to evaluate compound potency, measuring the half-maximal inhibitory concentration (IC-50) as a primary parameter, enabling precise assessment of inhibitor efficacy for drug development targeting CDK7 in Lupus Erythematosus.

Pharmacological Activity Material Method Parameter
Serine/threonine protein kinase (cdk7), inhibition Recombinant human enzyme ATP assay IC-50
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