Subtitle: Market Intelligence, Clinical Progress, and High-Purity Reagents for Innate Immunity, Interferonopathy, and Immuno-Oncology Development.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for cGAS/STING pathway drug discovery. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen (Wild-Type) | cGAS (MB21D1) Full-Length Recombinant Protein Sequence Verified, High Purity (>95%), Theoretical MW: 58.3 kDa. E. coli expressed (Active Enzyme). Endotoxin <1EU/ug. |
View cGAS Products |
| Antigen (Catalytic Mutant) | cGAS E225A/D227A Double Mutant Catalytically inactive (cGAMP synthesis deficient). For DNA-binding assays without enzymatic interference. |
View cGAS Products |
| Antigen (DNA-Binding Mutant) | cGAS K384A/K414A Mutant Deficient in DNA recognition. For studying catalytic activity independent of DNA activation. |
View cGAS Products |
| Gene Delivery | cGAS Promise-ORF Lentivirus Full-length ORF for stable cell line generation in HEK293 or THP-1. Endotoxin Controlled. |
View cGAS Products |
| Benchmark Antibody | Anti-cGAS (Clone 4A5 Recombinant) High-affinity mouse monoclonal, validated for Western Blot and IP. |
View cGAS Products |
| Validator | cGAS siRNA Set (3 target-specific + 1 control) For knockdown verification in cellular reporter assays. |
View cGAS Products |
| Related Target A: STING1 | STING1 (TMEM173) Recombinant Protein & Antibodies Downstream signaling node; essential for cGAMP sensing assays. |
View STING1 Products |
| Related Target B: ENPP1 | ENPP1 Recombinant Protein Hydrolyzes cGAMP; critical negative regulator and emerging synergistic target. |
View ENPP1 Products |
| Related Target C: TBK1 | TBK1 Kinase Recombinant Protein For phosphorylation cascade studies and compound selectivity screening. |
View TBK1 Products |
Critical Assay Challenge vs TarMart Advantage
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| Need to Distinguish DNA-Binding vs Catalytic Inhibition | Matched WT and Mutant Panel (E225A/D227A & K384A/K414A) strictly verified by mass spectrometry for precise MOA determination. |
| Enzymatic Activity Requires Functional Oligomerization | High-purity (>95%) full-length protein showing DNA-dependent dimerization confirmed by analytical SEC (Theoretical Oligomeric State). |
| Cross-Species Preclinical Translation (Human/Mouse/Cyno) | Ortholog proteins available for Human, Mouse, and Cynomolgus with sequence identity >85% for SAR studies. |
| Cellular Validation of Target Engagement | Lentivirus ORF particles for stable overexpression, paired with sequence-verified siRNA for specific knockdown controls. |
| Lack of Reliable Assay Controls (Biochemical Activity) | High Purity (>95%), properly folded recombinant cGAS optimized for enzymatic turnover assays. |
Live cGAS R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
- ➤ View Active Clinical Trials
- ➤ Latest SLE & Interferonopathy Research
- ➤ Latest Resistance Research
- ➤ Recent Patent Filings
Global Clinical Landscape & Future Outlook
The race for cGAS-targeted therapeutics is rapidly diversifying. Initial focus heavily favored cGAS-STING pathway activation for immuno-oncology, but a massive shift is occurring toward cGAS inhibitors for severe autoimmune and inflammatory conditions (such as Aicardi-Goutières syndrome and SLE). Novartis is advancing NDI-101150 (Phase II for SLE), and multiple biotechs (IFM Therapeutics, Ventus Therapeutics, Nimbus) are exploring neuroinflammation applications. The modality is shifting from pan-STING pathway inhibition to selective cGAS blockade to preserve beneficial immune responses.
Future waves indicate a surge in PROTAC-based cGAS degraders for durable pathway shutdown (e.g., Arvinas, Cullgen preclinical) and blood-brain barrier penetrant small molecules for Alzheimer's and Parkinson's disease (microglial cGAS inhibition). First-generation small molecules entering the clinic are being followed by next-wave R&D targeting highly selective allosteric inhibitors and combination therapies to modulate the innate immune microenvironment without systemic toxicity.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Small Molecule Inhibitor | Novartis, Ventus Therapeutics, Jiangsu Hengrui, Merck, GSK | SLE, Aicardi-Goutieres Syndrome (AGS) | Enzymatic Activity (cGAMP ELISA/HTRF); Need active WT protein & catalytic mutants for counter-screening |
| Small Molecule Agonist | GSK, Novartis | Solid Tumors (I-O) | Binding / Activation Kinetics (Need Sequence Verified protein panels) |
| PROTAC/Degrader | Arvinas, Cullgen (preclinical) | Refractory Interferonopathies | Cell-based degradation assays; Need lentivirus for stable cGAS-expressing reporter lines |
| Allosteric Inhibitor (Dimerization) | Academic/Pharma consortia | Neuroinflammation | Oligomerization assays (SEC, BLI); Need DNA-binding mutants to isolate protein-protein interactions |
| Targeted Protein Degraders | Nurix, Kymera | Oncology (TME modulation) | Selectivity panel vs TBK1/STING1; Need homologous pathway proteins |
| Gene Therapy / Degraders | Emerging Biotechs | Neuroinflammation | Cellular Depletion Assays (Need Lentivirus/siRNA for robust cell lines) |
Key Mutations and Research Tools
The cGAS protein (UniProt Q8N884) carries several clinically relevant mutations. Notable examples include dbSNP rs9352000 (VAR_050811) and rs610913 (VAR_033677), which are cataloged in the UniProt entry. A dominant mutation found in patients with tumors results in reduced nucleotidyltransferase activity, underscoring the importance of catalytic mutants for assay development. TarMart offers matched wild-type and mutant panels (including catalytic-dead E225A/D227A and DNA-binding-deficient K384A/K414A) to support precise mechanism-of-action studies. These tools are essential for differentiating competitive, non-competitive, and allosteric inhibitors in drug discovery programs.