PIK3R2 Drug Discovery Landscape & Assay Solutions

Phosphoinositide-3-Kinase Regulatory Subunit 2 (PIK3R2, also known as p85-beta) is a critical regulatory component of the Class IA PI3K pathway. By stabilizing the p110 catalytic subunit and mediating its recruitment to activated receptor tyrosine kinases (RTKs), PIK3R2 serves as a molecular switch in oncogenic signaling, metabolic regulation, and developmental disorders. As therapeutic strategies shift toward isoform-selective PI3K modulation and targeted protein degradation (PROTACs), high-purity reagents are essential to resolve the structural complexities of the PI3K regulatory-catalytic interface.

TarMart Solution Ecosystem & Related Targets

"Comprehensive reagent toolkit for PIK3R2 drug discovery. Select your modality below:"

Component / Network Product Description Product Link
Antigen PIK3R2 Recombinant Protein
High purity (>95%), Endotoxin <1EU/ug. Sequence Verified. Theoretical MW confirmed by SDS-PAGE. Suitable for biochemical interaction and structural studies.
View PIK3R2 Products
Gene Delivery PIK3R2 Promise-ORF / Lentivirus
Full-length ORF for stable cell line generation, enabling downstream AKT phosphorylation readouts in native cellular contexts.
View PIK3R2 Products
Benchmark Ab Anti-PIK3R2 Recombinant Antibody
Sequence-verified positive control for Western Blot, ELISA, and immunoprecipitation assays.
View PIK3R2 Products
Validator PIK3R2 siRNA Set
Target-specific siRNA sequences for functional knockdown verification and pathway specificity controls.
View PIK3R2 Products
Related Target A PIK3CA
The catalytic subunit p110-alpha. Co-targeting or co-expressing p110-alpha with PIK3R2 is essential for reconstituting active Class IA PI3K enzyme complexes.
View PIK3CA Products
Related Target B PIK3R1
The p85-alpha regulatory subunit. Critical for counter-screening and selectivity profiling to avoid off-target metabolic toxicity.
View PIK3R1 Products
Critical Assay Challenge The TarMart Advantage (Technical Spec)
Resolving p85α (PIK3R1) vs. p85β (PIK3R2) Selectivity Highly purified, sequence-verified homologous protein panels for precise off-target counter-screening.
Reconstituting Functional heterodimers High-purity recombinant PIK3R2 and catalytic partners (PIK3CA) expressed with native-like post-translational profiles.
Lack of Controls Sequence-verified clinical benchmark antibodies and recombinant positive controls included.
False Positives in Screening Multi-sequence validated siRNA knockdown pools included for target-specific validation.

Live PIK3R2 R&D Tracker

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

Global Clinical Landscape & Future Outlook

The race for PI3K pathway therapeutics is intensifying, with major players shifting focus from pan-PI3K inhibitors to isoform-selective modulators and targeted protein degraders (PROTACs). While early-generation pan-inhibitors faced dose-limiting toxicities—often due to off-target inhibition of PIK3R1-associated metabolic pathways—the next wave of R&D targets the regulatory subunit PIK3R2 to selectively disrupt oncogenic scaffolding without perturbing systemic glucose homeostasis. Disrupting the specific interaction between PIK3R2 and its catalytic partners represents a highly selective therapeutic window in solid tumors overexpressing p85-beta.

Competitive Modality & Indication Snapshot

Modality Representative Players Key Indications Critical Assay Need (Why TarMart?)
Small Molecule (PPI Inhibitors) Novartis, Genentech, Academic Consortia Breast Cancer, Endometrial Cancer, MPPH Syndrome Selectivity Assay (Need high-purity PIK3R2 vs. PIK3R1 proteins to verify isoform-specific disruption)
PROTACs / Degraders Arvinas, Kymera Therapeutics, Seed Therapeutics Refractory Solid Tumors, Lymphomas Ubiquitination & Binding Kinetics (Need sequence-verified PIK3R2 for SPR/FP ternary complex assays)
RNAi / Antisense Alnylam Pharmaceuticals, Ionis Pharmaceuticals Megalencephaly-Polymicrogyria (MPPH) Knockdown Validation (Need Lentivirus for stable cell lines and validated siRNA validation controls)