HSP90 Screening and Profiling

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Overview

As anti-cancer drug development increasingly moves toward precise, mechanism-driven strategies, targeting molecular chaperones has emerged as a key focus for many innovative therapeutic programs. Heat Shock Protein 90 (HSP90), one of the most critical chaperones in cellular stress response, plays a central role in stabilizing a wide range of client proteins involved in cell growth, proliferation, and signal transduction. Beyond maintaining protein folding and conformational balance, HSP90 is tightly linked to the aberrant signaling networks upon which tumor cells heavily rely. Consequently, the screening and functional profiling of HSP90 inhibitors have proven to be of high research value in oncology drug development.

HSP90 Screening and Profiling Figure 1. Diagram of HSP90 dimer showing its three domains with the ATP-binding pocket highlighted. (Magwenyane AM, et al., 2022)

Based on years of protein screening platform expertise, Creative Biogene has established a mature HSP90 Screening & Profiling platform. Leveraging high-purity recombinant protein production, ATPase activity assays, isoform-specific screening systems, and multi-mode mechanism validation assays, this platform enables researchers to rapidly generate high-quality screening results and accelerate the discovery and validation of lead compounds.

Background

HSP90 is a highly conserved molecular chaperone that becomes strongly upregulated under heat, oxidative stress, nutrient deprivation, toxins, or protein misfolding. It stabilizes numerous metastable client proteins, including over 50 oncogenic regulators such as AKT, HER2, EGFR, CDK4/6, and VEGFR. Blocking HSP90 triggers rapid client protein degradation via the ubiquitin–proteasome pathway, dismantling key survival signaling networks in tumor cells.

Early inhibitor discovery centered on N-terminal ATP-binding–site blockers like geldanamycin and 17-AAG, while newer strategies target the C-terminal domain or disrupt HSP90 dimerization to improve selectivity and reduce stress-response activation. For advancing HSP90 inhibitor programs, precise assessment of binding specificity, isoform selectivity (HSP90α vs. HSP90β), and downstream mechanistic effects remains essential—areas where Creative Biogene's platform provides robust and comprehensive support.

Features of Creative Biogene's HSP90 Screening & Profiling Services

Leveraging extensive protein screening experience, our platform offers comprehensive HSP90 analysis systems tailored to diverse research needs:

High-Purity Recombinant HSP90α/HSP90β and Client Protein Models: Suitable for conventional inhibitor screening and mechanism validation.
ATPase Activity Assays: Rapid evaluation of inhibitor potency and mechanistic characterization.
C-Terminal and Novel Mechanism Screening: Designed for early discovery of innovative lead molecules.
High-Throughput Screening Capabilities: Single-point concentration assays, IC₅₀ determination, and full inhibition curve analysis.
Isoform Selectivity Analysis: Comparative assessment of HSP90α and HSP90β inhibitor activity.
Client Protein Stability and Degradation Assays: Optional expansion to cell-based assays.
Target–Inhibitor Interaction Validation: Assessment of binding affinity, conformational impact, and mechanistic effects.

All experiments are conducted under strict quality control, ensuring stable, reproducible data suitable for integration into drug discovery workflows.

Creative Biogene HSP90 Screening & Profiling Services

Our HSP90 Screening & Profiling services provide comprehensive support for all stages of drug discovery, from high-throughput early screening to mechanistic validation and candidate evaluation. Key features include:

Diverse Assay Options

ATPase inhibition testing
HSP90 complex stability assessment
Client protein degradation monitoring
Isoform-selectivity comparison
N-/C-terminal inhibition mechanism analysis

High-Quality Experimental Platform

Purified protein systems
Optional HSP90 inhibitor libraries
Comprehensive quantitative analysis with fully customizable workflows

Precise Mechanistic Insights

Systematic concentration–response analyses generating accurate IC₅₀ values and curve-fitting parameters
Assessment of client protein stability changes to elucidate compound mechanisms

Isoform-Selective Profiling & Optimization

Parallel screening of HSP90α and HSP90β
Isoform-selective data supporting SAR studies and compound optimization

Innovative Inhibitor Evaluation

Analysis of novel mechanisms, such as potential C-terminal targeting molecules
Binding and interference evaluation to enable the discovery of innovative inhibitory strategies

Actionable Data & Research Value

End-to-end support from early-stage screening to candidate validation
High-quality data and in-depth analyses accelerate decision-making, saving time and resources in drug development

Deliverables and Data Format

Upon project completion, clients receive:

Detailed experimental reports and assay descriptions
ATPase inhibition data, inhibition curves, IC₅₀ values, and fitted parameters
Isoform selectivity comparative analysis (if applicable)
Client protein stability or degradation results (optional)
Mechanistic insights and inferred inhibitory modes (based on experimental combination)

All data are delivered in standardized electronic formats suitable for internal R&D review, regulatory submissions, or further SAR analysis.

Why Choose Creative Biogene

With a mature protein screening platform, a professional drug discovery team, and robust, controlled experimental systems, Creative Biogene ensures high-quality, reproducible data while shortening screening timelines. Our expertise spans inhibitor screening, isoform selectivity analysis, and mechanistic validation, with highly customizable services adaptable to any stage of research.

Whether developing HSP90-targeted inhibitors, exploring novel mechanisms, or requiring systematic profiling data to advance projects, Creative Biogene provides the expertise and resources to accelerate high-quality lead discovery and support your drug development efforts.

* For research use only. Not intended for any clinical use.

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