SMARCA2 Drug Discovery Landscape & Assay Solutions

TarMart Solution Ecosystem & Related Targets

Component / Network Product Description Product Link
Biochemical Antigen SMARCA2 Full-Length & ATPase Domain Proteins
High purity (>95%), Endotoxin <1EU/μg, Sequence Verified, HEK293 Expressed (Native Glycosylation), Theoretical MW confirmed.
View SMARCA2 Products
Gene Delivery SMARCA2 Promise-ORF Lentivirus
Full-length ORF for stable cell line construction and synthetic lethality validation.
View SMARCA2 Products
Detection Antibody Anti-SMARCA2 (Research Grade)
For Western Blot, Co-IP, and ternary complex detection. Sequence of clone verified.
View SMARCA2 Products
Validator SMARCA2 siRNA Set
For knockdown and synthetic lethality verification. Sequence-verified targets.
View SMARCA2 Products
Synthetic Lethality Pair SMARCA4 (BRG1)
Essential for selectivity profiling and counter-screening; 80% homology requires matched reagents.
View SMARCA4 Products
Complex Component SMARCB1 (INI1)
Core SWI/SNF subunit for complex assembly and protein-protein interaction assays.
View SMARCB1 Products
Critical Assay Challenge The TarMart Advantage (Technical Spec)
ATPase Activity & Binding Affinity Full-length SMARCA2 with intact ATPase domain (>95% purity, Sequence Verified by Mass Spec, Endotoxin <1EU/μg)
SMARCA4 Selectivity (High Homology) Matched pair of SMARCA2 & SMARCA4 proteins from same HEK293 batch; sequence-verified distinct epitopes for antibody selectivity testing
PROTAC Ternary Complex Formation High-concentration protein formulation (>5 mg/mL) suitable for crystallography and SPR/ITC analysis
False Positives in Cellular Assays Validated siRNA included for specificity checks; Lentivirus for stable expression controls

Key Functional Domains and Mutations

SMARCA2 (BRM) contains several conserved functional domains essential for chromatin remodeling:

  • QLQ domain: Involved in protein-protein interactions, important for SWI/SNF complex assembly.
  • HSA (Helicase/SANT-Associated) domain: Mediates interactions with other complex components.
  • Helicase ATP-binding domain: Core enzymatic domain responsible for ATP hydrolysis and chromatin remodeling activity.

Key mutations identified in patients:

  • VAR_085660: Found in a patient with non-specific intellectual disability syndrome; likely pathogenic.
  • VAR_085661: Found in a patient with non-specific intellectual disability syndrome; likely pathogenic.
  • VAR_085662: In BIS (Coffin-Siris syndrome), affecting the SWI/SNF complex function.

These mutations highlight the critical role of SMARCA2 in neurodevelopment and tumor suppression.

Global Clinical Landscape & Future Outlook

The race for SMARCA2 therapeutics is intensifying, with major players shifting focus from traditional small molecule inhibitors to targeted protein degraders (PROTACs/Molecular Glues). First-generation PROTACs (e.g., CFT-1945) are entering Phase I trials for SMARCA4-mutant NSCLC, while the field rapidly pivots toward paralog-selective degradation and combination strategies to circumvent acquired resistance. With SMARCA4 mutations prevalent in lung, ovarian, and pancreatic cancers, synthetic lethality biomarkers position SMARCA2 as a dominant oncology target. Moreover, patient-derived mutations in SMARCA2 (e.g., those causing intellectual disability and BIS) highlight the need for isoform-selective therapies to avoid on-target toxicity.

Competitive Modality & Indication Snapshot

Modality Representative Players Key Indications Critical Assay Need (Why TarMart?)
PROTAC Degraders C4 Therapeutics, Cascade Therapeutics, Prelude Therapeutics SMARCA4-mutant NSCLC, Small Cell Ovarian Carcinoma Ternary Complex Assembly (Need high-purity full-length protein & E3 ligase components)
ATPase Inhibitors (Dual/Single) Foghorn Therapeutics, Bayer, Foresight Diagnostics SMARCB1-deficient Tumors, Solid Tumors Enzymatic Activity & Selectivity (Need active ATPase domain vs SMARCA4 counter-screen)
Molecular Glues Undisclosed Biotech Partnerships SWI/SNF Dysregulated Cancers Protein-Protein Interaction Disruption (Need SMARCB1 complex reconstitution)
Synthetic Lethal Combinations Academic & Industry Consortia Pancreatic, SMARCB1-null tumors Rescue / Knockdown Assay (Need ORF lentivirus + siRNA validators)

Live SMARCA2 R&D Tracker

Market data changes daily. Access the latest global pipeline status directly:

Related Target Note

Beyond SMARCA4 and SMARCB1, ARID1A is a core SWI/SNF complex subunit frequently co-mutated in solid tumors, making it an important target for combination studies. TarMart provides ARID1A reagents (see View ARID1A Products).