Market Intelligence, Clinical Progress, and High-Purity Reagents for Metabolic Disease and Oncology Development.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for PRKAA2 drug discovery. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen | PRKAA2 Kinase Domain & Mutant Proteins High purity (>95%), Endotoxin <1EU/ug. Sequence Verified. Includes T172D (Constitutively Active) and D157A (Kinase Dead). |
View PRKAA2 Products |
| Gene Delivery | PRKAA2 Lentivirus Premade Particles Full-length ORF with HA-tag for stable cell line construction. Constitutively active mutant available. |
View PRKAA2 Products |
| Benchmark Ab | Anti-PRKAA2 (Pan-Specific) & Phospho-Thr172 High-affinity research grade antibody for Western/IF. |
View PRKAA2 Products |
| Validator | PRKAA2 siRNA Set Three unique targets for knockdown verification. Sequence-verified. |
View PRKAA2 Products |
| Isoform Control | PRKAA1 (AMPK Alpha 1) Essential for selectivity screening vs. Alpha 2 isoform. |
View PRKAA1 Products |
| Complex Partner | PRKAB2 (AMPK Beta 2) Regulatory subunit for holoenzyme reconstitution assays. |
View PRKAB2 Products |
| Pathway Node | STK11 (LKB1) Upstream activator kinase. Critical for pathway validation. |
View STK11 Products |
| Downstream Substrate | ACC1 (Acetyl-CoA Carboxylase 1) Direct functional readout for AMPK activation; phosphorylation at Ser79 is the PD marker. |
View ACC1 Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| Isoform Selectivity (Alpha 2 vs Alpha 1) | Human PRKAA2 and PRKAA1 catalytic domains available side-by-side; HEK293 expressed (>95% purity); Sequence Verified for ATP-binding cleft identity. |
| Constitutive Activity Modeling | T172D Phospho-mimetic mutant (mimics Thr172 phosphorylation) available for functional gain-of-study; Theoretical MW confirmed by Mass Spec. |
| Holoenzyme Assembly & Regulation | Compatible with PRKAB and PRKAG subunits for heterotrimeric complex reconstitution; Native glycosylation preserved (HEK293 system). |
| Specificity & Negative Controls | Kinase-dead D157A mutant + validated siRNA set included; Endotoxin controlled (<1 EU/μg) for cellular assay integrity. |
Global Clinical Landscape & Future Outlook
The race for PRKAA2-targeted therapeutics is intensifying, with major players shifting focus from pan-AMPK activation (e.g., metformin, AICAR) to Alpha 2-selective modulation. Following the discontinuation of first-generation direct activators (e.g., Merck's MK-8722) due to cardiac hypertrophy concerns, the next wave of R&D targets tissue-specific delivery—primarily skeletal muscle for metabolic disease and hepatic/tumor-specific contexts. Second-generation allosteric modulators (e.g., Poxel's PXL770) and indirect activators (via LKB1/STK11 pathway) are entering the clinic. Major indications include Type 2 Diabetes, NASH, chronic kidney disease, and LKB1-deficient tumors. The demand for rigorous isoform selectivity assays, holoenzyme reconstitution tools, and mutant-specific validation has become the primary technical bottleneck for lead optimization.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Direct Alpha 2 Activator (Small Mol) | Merck (legacy), Calico/Gilead, AstraZeneca | Type 2 Diabetes, NASH | Isoform Selectivity Assay (Need purified PRKAA2 vs PRKAA1 catalytic domains with native folding) |
| Indirect Activator (Allosteric) | Poxel, Immuneering, Academic Consortia | NASH, Cachexia, Metabolic Syndrome | Holoenzyme Conformational Assay (Need full-length PRKAA2 + PRKAB/PRKAG subunits) |
| PROTACs / Degraders | Emerging Biotechs | Oncology (Context-dependent, LKB1-deficient) | Degradation & Synthetic Lethality Assays (Need specific antibodies and stable cell lines via Lentivirus) |
| Gene Therapy | Academic/Translational Spin-offs | Cardiovascular Aging, Metabolic Disease | Expression Validation (Need strictly verified ORF/Lentivirus) |
Key Mutations and Clinical Relevance
PRKAA2 is a protein kinase (functional domain confirmed by UniProt). Several somatic mutations have been identified in cancer samples:
- Breast cancer (infiltrating ductal carcinoma) – somatic mutation (VAR_035623)
- Gastric adenocarcinoma – somatic mutation (VAR_040355)
- Breast cancer – somatic mutation (VAR_035624)
These mutations may influence drug binding, kinase activity, or downstream signaling. Researchers developing selective modulators should consider these variants in resistance profiling and patient stratification. TarMart offers custom mutagenesis services to generate relevant mutant proteins for preclinical evaluation.
Live PRKAA2 R&D Tracker
Market data changes daily. Access the latest global pipeline status directly: