PROTAC GSPT1 degrader-1 , CAS No.3034310-17-0

CAS: 3034310-17-0 Cat. No.: P1448700 Formula: C₃₇H₃₆ClN₇O₅ Molecular Weight: 694.18

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

PROTAC GSPT1 degrader-1 (Compound F) is a PROTAC degrader for G1 to S phase transition protein 1 ( GSPT1 ) that degrades GSPT1 with a rate of 95% (1 μM) GSPT1 and 86% (0.1 μM). PROTAC GSPT1 degrader-1 inhibits the cell viability of HL-60 with an IC 50 of 9.2 nM. (Pink: ligand for target protein ; Black: linker ; Blue: ligand for E3 ligase )

Specifications

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Names and Identifiers

Molecular Weight

694.18

Application Protocols

No manufacturer-validated protocols are provided for this item. The following are general, non-item-specific considerations for small-molecule PROTAC tools; users must optimize for their systems.

• Stock solution: Dissolve in anhydrous DMSO to 10–50 mM. Vortex and, if needed, sonicate briefly. Filter if particulate remains (PTFE, 0.2 µm). Aliquot and store at −20°C.
• Cell-based assays (general): Titrate across a broad range (e.g., 1 nM to 10 µM final), maintaining constant DMSO (≤0.1–0.5%). Include negative controls (vehicle; ligase binder alone; target binder alone) and positive controls if available. Assess degradation by immunoblot at multiple time points (e.g., 2, 6, 24 h). Confirm proteasome dependence with MG132 or epoxomicin controls where appropriate.
• Biochemical/biophysical assays: Use TR-FRET, CETSA, or pulldown-based methods to probe ternary complex formation and target engagement.
• Data quality: Monitor cytotoxicity separately from degradation to disentangle primary effects. Consider proteomics for off-target assessment.

Note: These are literature-based best practices, not product-validated methods.

Biological Roles

General background (literature; not item-specific performance):

• PROTACs drive targeted protein degradation by promoting formation of a ternary complex between an E3 ubiquitin ligase and a protein of interest, leading to ubiquitination and proteasomal degradation.
• GSPT1 (also known as eRF3A) is a GTP-binding protein involved in translation termination and mRNA surveillance pathways. Its degradation has been studied to probe cellular translation control and for target validation in oncology research settings.
• Typical readouts for PROTACs aimed at GSPT1 include time- and concentration-dependent loss of GSPT1 protein, downstream pathway modulation, and cellular viability changes in sensitive models. Confirm effects with orthogonal assays (e.g., rescue with proteasome inhibitor, evaluation of neosubstrate specificity, or genetic controls).

Important caveats:

• This item’s exact binding elements (E3 ligase recruiter, target warhead) and potency/selectivity profile are not specified. Empirical verification in the user’s system is essential.
• Cellular uptake, efflux, metabolic stability, and potential for off-target degradation can vary markedly with linker architecture; titrate conditions and verify by proteomics where feasible.

Buffer Applications

This compound is not a buffering agent. However, buffers are relevant for its use in biological assays.

Practical guidance (general for PROTAC tools):

• Stock preparation: Dissolve in DMSO to 10–50 mM. Store aliquots at −20°C. Thaw on ice and use promptly.
• Aqueous dilution: Dilute stocks into assay buffers such as PBS (pH 7.2–7.4) or HEPES-buffered media while maintaining a low final DMSO fraction (e.g., 0.05–0.5%). Mix thoroughly to avoid local supersaturation.
• Additives: To reduce nonspecific adsorption and precipitation, include 0.1–0.5% fatty-acid–free BSA or 0.01% nonionic surfactant (e.g., Tween-20), if compatible with the assay.
• Stability checks: After dilution, visually inspect for precipitation; optionally confirm by quick spin and UV absorbance at a non-interfering wavelength or by LC.

Note: Item-specific solubility and stability in buffers are not specified; validate compatibility in your assay matrix.

Green Alternatives

While green chemistry frameworks typically address process solvents and reagents, some considerations apply to handling this research compound.

• Stock solvent choices (general guidance): Prefer DMSO or ethanol over halogenated solvents. Where feasible, use water-miscible systems to enable rapid dilution into aqueous buffers.
• Formulation strategies: Use minimal organic solvent by preparing higher concentration stocks and diluting to the lowest effective final organic percentage in assays (e.g., ≤0.1–0.5% DMSO).
• Waste minimization: Plan experiments to minimize excess solution preparation; employ microscale assay formats (96/384-well) to reduce solvent use.

Comparison of common stock solvents (general):

• DMSO: high solvency; relatively low volatility; acceptable EHS profile in small-scale research use; avoid >0.5–1% in live-cell assays.
• Ethanol: renewable feedstocks possible; lower solvency for bulky PROTACs; higher volatility.
• DMF/NMP: strong solvency but less favorable EHS; reserve for stock preparation when necessary and handle in a fume hood.

Note: No greener “alternative compound” is applicable here because the molecular identity and performance are fixed; focus sustainability efforts on solvent selection, right-sizing, and responsible waste handling.

Pharmaceutical Uses

No pharmacopeial status or excipient role is provided for this item.

Context for research (general, non-clinical):

• PROTACs are widely used in drug discovery to validate targets and mechanisms by degradation rather than occupancy. Compounds that degrade GSPT1 have been explored in oncology research to study translation termination pathways. This product is supplied strictly for laboratory research and method development; it is not intended for therapeutic, diagnostic, or clinical use.
• Formulation experiments in discovery can investigate solubilization approaches (e.g., DMSO-based dilutions, PEG400/ethanol/water cosolvent systems, cyclodextrins) to support in vitro or ex vivo testing. Any in vivo formulation or dosing would require institutionally approved protocols and compound-specific data, which are not provided here.

Physical Properties

Item-specific physicochemical data are not provided.

• Appearance: Not specified for this item; refer to CoA/Spec Sheet.
• Melting point: Not specified for this item; refer to CoA/Spec Sheet.
• Boiling point: Not applicable for most PROTAC solids; specific value not specified for this item; refer to CoA/Spec Sheet.
• Density: Not specified for this item; refer to CoA/Spec Sheet.
• Solubility: Not specified for this item; refer to CoA/Spec Sheet.
• LogP/logD: Not specified for this item; refer to CoA/Spec Sheet.
• pKa: Not specified for this item; refer to CoA/Spec Sheet.
• Refractive index: Not applicable (typically a solid); not specified for this item.

General guidance (literature, PROTAC class):

• PROTACs often exhibit high polarity and molecular weight, with limited aqueous solubility. DMSO stocks (e.g., 10–50 mM) are commonly used for in vitro work, followed by dilution into assay buffers containing carrier protein (e.g., 0.1–0.5% BSA) to mitigate adsorption.
• Solubility can be formulation-dependent; co-solvents (PEG400, ethanol), cyclodextrins, or micellar systems are sometimes employed in discovery research. Validate experimentally for this specific item.

Quality & Grades

• Grade/Purity: Not specified for this item; refer to CoA/Spec Sheet for exact purity, analytical methods, and residual solvent limits.

Context and expectations (general for screening compounds/PROTAC tools):

• Discovery-grade small molecules are typically supplied at high chemical purity (e.g., ≥95% by HPLC/LC-MS), but the exact value, assay wavelength, and chromatographic conditions must be confirmed on the CoA for this specific SKU.
• Identity verification is commonly supported by LC–MS and/or NMR. If orthogonal confirmation is required (e.g., HRMS, elemental analysis, chiral HPLC), request the corresponding documentation.
• Stabilizers: None specified for this item. If present, stabilizers would be listed on the CoA/SDS; their presence can influence solubility and bioassays.
• Batch consistency: For structure–activity studies, use a single lot when possible, or cross-qualify lots by re-characterizing purity/identity under your in-house methods.

Reaction & Applications

This material is a bioactive research tool (PROTAC) and is not typically used as a reagent or catalyst in synthetic transformations. Consequently, classic synthetic reaction families (e.g., cross-coupling, reductions) are not the primary use-case for this item.

Applicable research applications (general for PROTAC tools; item-specific performance not specified):

• Targeted protein degradation studies in biochemical or cellular systems, focusing on modulation of GSPT1 pathways. Validate degradation by immunoblotting or proteomics; confirm dose–response and time-course.
• Mechanistic assays to explore ternary complex formation with an E3 ubiquitin ligase and the putative target protein.
• Chemoproteomics or CETSA/thermal shift experiments to infer target engagement.

Notes:

• Because item-specific potency, selectivity, and cell permeability are not provided, users should establish their own assay conditions and positive/negative controls. Include appropriate DMSO controls and, when possible, orthogonal chemistry comparators (inactive analogs, ligase binder alone, target binder alone).

Reaction Conditions

Not applicable. This product is not intended as a reagent for synthetic transformations, and no reaction condition guidance is relevant.

For experimental use as a research tool compound, see the Solvent Selection, Biological Roles, and Application Protocols sections for handling and assay-related considerations.

Safety & Handling

• GHS classification: Not specified for this item; refer to SDS.
• Signal word / H-Statements / Pictograms: Not specified for this item; refer to SDS.
• Research use: For research use only (not for human or veterinary use).
• Storage: Store at −20°C (from product data). Minimize freeze–thaw cycles by preparing aliquots.
• Shipping: Ice chest + ice pads (from product data).

General laboratory precautions (good practice; defer to SDS as authoritative):

• PPE: Lab coat, safety glasses, and appropriate chemically-resistant gloves. Handle powders in a fume hood to avoid inhalation and cross-contamination.
• Incompatibilities: Avoid strong oxidizers and strong acids/bases unless compatibility is known (general precaution for organic bioactive small molecules).
• Preparation: Open vials at ambient humidity/temperature conditions that minimize condensation. Allow to equilibrate to room temperature in a desiccator before opening to prevent moisture uptake.
• First aid (general): In case of contact, rinse with water for 15 minutes; remove contaminated clothing. If inhaled, move to fresh air. Seek medical attention if any adverse effects occur. Always consult the SDS for item-specific measures.
• Waste: Dispose according to institutional and local regulations for organic research chemicals.

Solvent Selection

Item-specific solubility data are not provided; consult the CoA or perform a small-scale solubility screen.

General guidance (literature, PROTAC class):

• Primary stock solvent: DMSO is typically preferred due to good solvating power for high-MW, polar, heteroatom-rich molecules. Prepare concentrated stocks (e.g., 10–50 mM) and store at −20°C in aliquots.
• Assay dilution: Dilute DMSO stocks into aqueous assay buffers (PBS, HEPES) while maintaining a low final DMSO fraction (e.g., ≤0.1–0.5%) to limit solvent effects. Include inert carrier protein (0.1–0.5% BSA) or low levels of nonionic surfactant (e.g., 0.01% Tween-20) to reduce adsorption and precipitation, if assay-compatible.
• Alternative solvents (if DMSO is unsuitable): DMF or NMP for stock preparation; ethanol or isopropanol for intermediate dilutions. Validate compatibility with biological assays.
• Solvent screening tips: Start with DMSO, then assess co-solvent blends (e.g., DMSO:PEG400:water) for higher concentrations. Visually inspect for clarity; confirm by UV or LC.

Comparison (general):

• DMSO: strongest solvency, broad assay compatibility; may affect cells/enzymes at >0.5–1% v/v.
• DMF/NMP: strong solvency; higher toxicity; typically limited to stock solutions.
• Ethanol: more benign but lower solvency for bulky PROTACs.

Storage & Reconstitution

• Storage temperature: Store at −20°C (from product data). Protect from light and moisture.
• Shipping: Ice chest + ice pads (from product data).
• Reconstitution solvent: Not specified for this item; refer to CoA/Spec Sheet. General practice for PROTACs is dissolution in anhydrous DMSO.
• Aliquoting: To avoid freeze–thaw degradation and adsorption losses, prepare single-use aliquots of stock solution (e.g., 10–50 mM in DMSO) in inert vials or low-bind tubes. Purge headspace with inert gas if long-term storage is anticipated.
• Handling: Allow vials to equilibrate to room temperature before opening to prevent condensation. After thawing an aliquot, keep on ice and use promptly.
• Stability: Item-specific stability (solid or in solution) is not specified; verify by LC–MS/HPLC after storage. Discard solutions showing precipitation, discoloration, or unexpected LC peaks.

Always consult the CoA and SDS accompanying your lot for definitive guidance on storage, stability, and handling.

Structure & Identity

Item-specific identifiers are scarce for this catalog entry. Where unavailable, consult the CoA/SDS.

• Product name: PROTAC GSPT1 degrader-1 (research tool compound)
• CAS: 3034310-17-0
• Molecular formula: Not specified for this item; refer to CoA/Spec Sheet.
• Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.
• SMILES: Not specified for this item; refer to CoA/Spec Sheet.
• InChIKey: Not specified for this item; refer to CoA/Spec Sheet.

General structural notes (literature, PROTAC class):

• PROTACs are typically heterobifunctional small molecules composed of two recognition ligands joined by a chemical linker.
  • One ligand binds an E3 ubiquitin ligase (commonly CRBN, VHL, MDM2, or cIAP; specific recruiter for this item is not specified).
  • The other ligand binds the protein of interest (here, GSPT1/eRF3A is implied by product name; exact warhead is not specified for this item).
• Typical 2D depiction: [E3 ligase binder]–linker–[target binder]; often high molecular weight, multiple heteroatoms, and potential chiral centers (literature/general for PROTACs).

Synthetic Utility

This material is a finished bioactive small molecule tool and is not typically used as a building block or reagent in synthetic chemistry.

General notes (PROTAC class, literature):

• PROTAC molecules are assembled from three modular components: an E3 ligase ligand, a target-binding ligand, and a linker. Synthetic routes often leverage amide couplings, click reactions (CuAAC), or ether/urea formations to connect modules.
• Without item-specific structure, further retrosynthetic discussion is not applicable. If custom derivatives or linkers are required for SAR exploration, consult the primary literature for synthetic strategies pertinent to the chosen ligase recruiter and target ligand scaffolds.

Target Specificity

No antibody or biologic attributes apply. Target specificity details (e.g., antigen/epitope, species reactivity, clone) are not applicable to this small-molecule product.

Item-specific biochemical target information beyond the product name is not provided; users should verify on-target degradation and off-target profiles empirically in their systems.

Frequently Asked Questions

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 3034310-17-0, the molecular formula is C37H36ClN7O5, and the molecular weight is 694.18 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.