Market Intelligence, Preclinical Progress, and High-Purity Reagents for Cytoskeleton-Targeted Therapy Development in Oncology and CNS.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for ARHGAP9 (RICS) drug discovery. Select your modality below for Rho GTPase regulation studies.
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen (Full-Length) | ARHGAP9 Recombinant Protein. HEK293 Expressed, Theoretical MW ~116 kDa, Sequence Verified, Endotoxin <1EU/µg. High purity (>95%). | View ARHGAP9 Products |
| Antigen (Domain) | ARHGAP9 BAR-RhoGAP Domain (1-350aa). Truncated construct for structural studies. | View ARHGAP9 Products |
| Catalytic Control | ARHGAP9 R143A Mutant Protein. Catalytically inactive GAP domain variant for negative control assays. | View ARHGAP9 Products |
| Gene Delivery | ARHGAP9 Lentivirus Particles. CMV promoter, Puromycin selection, for stable cell lines. | View ARHGAP9 Products |
| Benchmark Ab | Anti-ARHGAP9 (Rabbit Recombinant mAb). Research-grade positive control for Western/IP. | View ARHGAP9 Products |
| Validator | ARHGAP9 siRNA Set (3 pre-designed). For knockdown verification and specificity controls. | View ARHGAP9 Products |
| Related Target | RHOA. Primary substrate GTPase; required for GAP activity assays. | View RHOA Products |
| Related Target | CDC42. Neuronal-specific substrate; critical for CNS indication validation. | View CDC42 Products |
| Related Target | RAC1. Direct downstream GTPase substrate; essential for GAP activity assays. | View RAC1 Products |
| Pathway Partner | CNTNAP2 (CASPR2). SH3-domain binding partner; synaptic function studies. | View CNTNAP2 Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| GTPase Activity Reconstitution (Rac1/Cdc42) | High-purity ARHGAP9 RhoGAP domain (>95%) for reliable catalytic turnover assays. |
| Selectivity vs. Paralog RhoGAPs (e.g., DLC1, ARHGAP1) | Full-length and domain-truncation panels; Sequence-verified orthologs. |
| Intracellular Target Engagement | Lentivirus-based stable overexpression/knockdown cell lines for target validation. |
| Off-Target Binding in Screening | Validated siRNA included for specificity checks; Benchmark antibody controls. |
| Catalytic Domain Integrity | HEK293 Expression System ensures mammalian glycosylation and proper BAR-domain conformation. |
| Specificity Control | Matched R143A Catalytic Dead Mutant available as rigorous negative control. |
| Neuronal Cell Line Generation | High-titer Lentivirus (>10^8 TU/ml) with Puromycin selection optimized for SH-SY5Y and primary neurons. |
| Substrate Co-purification | Low Endotoxin (<1EU/µg) enables sensitive cellular assays without LPS interference. |
Live ARHGAP9 R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Global Clinical Landscape & Future Outlook
The race for ARHGAP9-targeted therapeutics is accelerating at the academic-biotech interface, with major emphasis shifting from broad cytoskeleton disruptors to precise RhoGAP modulation, including protein-protein interaction (PPI) disruptors and targeted degradation strategies. ARHGAP9 (also known as RICS or BPGAP1) is a Rho GTPase-activating protein containing BAR, RhoGAP, SH3, WW, and PH domains. It negatively regulates RhoA, Cdc42, and Rac1, playing critical roles in neuronal axon guidance, synaptic plasticity, tumor cell migration, and immune cell infiltration. Schizophrenia GWAS data robustly links ARHGAP9 loci to disease risk, and oncology studies demonstrate its role in metastasis suppression in gliomas. The next wave of R&D focuses on CNS-penetrant modulators and metastasis-prevention combinations. Currently, no ARHGAP9-specific drug has entered clinical trials; the field is dominated by academic consortia and early-stage biotechs exploring small molecule inhibitors, PROTACs, siRNA, and peptide modalities. Known missense mutations (e.g., rs33927108, rs3802989, rs11544238) have been cataloged in dbSNP, providing potential biomarkers for precision medicine. The primary indications include refractory solid tumors (glioma, triple-negative breast cancer, hepatocellular carcinoma) and CNS disorders (schizophrenia, cognitive deficits).
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Small Molecule Inhibitors (PPI) | Academic Consortia, CNS-focused Biotech | Metastatic Solid Tumors, Schizophrenia, Cognitive Deficits | GTPase turnover assay (Need high-purity ARHGAP9 GAP domain); Full-length BAR-GAP Protein for binding assays; Mutant controls for specificity. |
| PROTAC / Molecular Glue | Early-stage platforms, Oncology Biotech | Refractory Carcinomas, Metastatic Glioma, Triple-Negative Breast Cancer | Target engagement assay (Need full-length protein & stable cell lines); Ternary complex formation (Need high-purity recombinant proteins). |
| siRNA / Gene Therapy | Specialty gene-silencing firms, Gene Therapy Platforms | Invasive Tumors, Rare CNS Disorders | Knockdown validation (Need validated siRNA & lentivirus rescue); Stable knockdown via shRNA vectors. |
| Peptide / Miniprotein | Biotech Startups | Neuroregeneration | SH3-domain specific truncations; Sequence-verified synthetic antigens. |
Key Assay Considerations & Molecular Differentiation
Based on ARHGAP9's domain architecture (SH3, WW, PH, and RhoGAP), assay strategies must address:
- Substrate specificity: ARHGAP9 acts on Cdc42 and Rac1 preferentially; RhoA is also regulated. Use specific GTPase loading controls.
- Selection against paralogs: The RhoGAP family has >70 members. Achieve >100-fold selectivity against ARHGAP1, ARHGAP24, etc., via cross-screening panels.
- Mechanism-based controls: Catalytic dead mutant (e.g., R143A) and domain-truncated versions (BAR-GAP, SH3 only) allow dissection of catalytic versus scaffolding functions.
- Cellular models: Use ARHGAP9 overexpressing or knockdown stable cell lines (lentivirus) for wound healing, Transwell invasion, and neurite outgrowth assays.
TarMart provides sequence-verified, high-purity (>95%) recombinant proteins (full-length, BAR-RhoGAP, RhoGAP-SH3), matched mutants, lentivirus particles, and validated siRNA sets to enable each of these critical assays.
Related Targets & Pathway Partners
- RHOA, CDC42, RAC1 – primary substrates for GAP activity assays.
- CNTNAP2 (CASPR2) – SH3-domain binding partner for synaptic function studies.
- DLC1 – parallel RhoGAP tumor suppressor for selectivity counter-screening.
- ARHGAP1 – family member for cross-reactivity profiling.
These reagents are available via TarMart's comprehensive catalog, supporting both oncology and CNS research.