≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Protected from light,Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Overview
GSK2647544 is an orally available, selective inhibitor of Lp-PLA2. Lipoprotein-associated phospholipase (Lp-PLA2) is a calcium-independent phospholipase A2 with proinflammatory activities that is primarily secreted by monocyte-derived macrophages.
Form:Solid
Specifications
Specifications & Purity
≥99%
Biochemical and Physiological Mechanisms
GSK2647544 is an orally available, selective inhibitor of Lp-PLA2 . Lipoprotein-associated phospholipase (Lp-PLA2) is a calcium-independent phospholipase A2 with proinflammatory activities that is primarily secreted by monocyte-derived macrophages.
Storage
Protected from light,Store at -80°C
Shipped In
Dry ice packs + Cold packs
This product requires cold chain shipping. Ground and other economy services are not available.
DMSO : 100 mg/mL (198.86 mM; ultrasonic and warming and heat to 60°C)
Solution Calculators
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Application Protocols
Item-specific, tested application protocols (WB, IHC, IF, FC, enzyme assays, cell-based assays): Not specified for this item; refer to CoA/Spec Sheet and internal method SOPs.
General protocol framework for small-molecule probe use (guidance only):
Biochemical enzyme assay:
Prepare a 10–50 mM DMSO stock; make serial dilutions to achieve a 10‑point concentration–response (e.g., 0.1 nM–30 µM final).
Keep final DMSO constant across wells (e.g., 0.5% v/v). Include vehicle controls and, if available, a known reference inhibitor.
Incubation times and substrate concentrations should be optimized for initial-rate conditions; monitor product formation by fluorescence, absorbance, or LC–MS.
Cell-based assay:
Confirm cytotoxicity window (e.g., 24–72 h viability) for your cell type and solvent level.
Dose over a range bracketing reported biochemical potency; consider serum binding by testing in both low- and high-serum conditions.
Sample preparation for LC–MS:
Quench with ACN (3–4× volume), add internal standard, centrifuge, and analyze supernatant using a water/ACN gradient with formic acid or ammonium formate.
Documentation:
Record lot number, stock concentration, solvent, preparation date, and storage history; attach CoA to data packages.
Biological Roles
Item-specific biological role: Not specified for this item; refer to CoA/Spec Sheet and primary literature before assigning functional annotations.
Literature context (for planning and hypothesis generation only; verify with original sources):
GSK2647544 has been reported as a potent, selective small-molecule inhibitor targeting a phospholipase A2–related enzymatic pathway, used as a chemical probe to modulate lipid mediator formation in biochemical and cellular systems. Researchers have employed such probes to study hydrolysis of phospholipids at the sn‑2 position and consequent bioactive lipid generation.
Experimental considerations:
When using as a probe, confirm target identity (enzyme isoform), Ki/IC50 values, mode of inhibition (competitive/noncompetitive), and selectivity panel against related lipases and off‑targets.
Assess time‑ and concentration‑dependent effects, reversibility, and potential aggregation or colloidal behavior via control assays (e.g., detergent sensitivity, dynamic light scattering at high micromolar concentrations).
ADME/PK (general, not item-specific):
For enzyme probes, permeability, plasma protein binding, and microsomal stability can markedly influence cellular versus biochemical potency; tailor assay design accordingly.
Caution:
Do not infer therapeutic effects from biochemical activity. This product is for research use only and is not intended for diagnostic or clinical use.
Buffer Applications
Applicability: This compound is not a buffer reagent. It does not establish a defined pH range or buffering capacity.
Practical guidance for use of this compound in buffered systems (general):
Prepare concentrated stock in DMSO (or other suitable solvent) and dilute into the target physiological buffer (e.g., HEPES, PBS) ensuring the final co‑solvent level is within assay tolerance (commonly ≤0.1–1% v/v DMSO).
To mitigate precipitation upon dilution, add the stock slowly with vigorous mixing, or pre‑mix with an equal volume of buffer prior to bulk addition.
If adsorption to plastics is suspected at low nM concentrations, consider low-bind tubes/plates and include small amounts of carrier protein (e.g., 0.1% BSA) if compatible with the assay.
For electrophysiology or other sensitive assays:
Validate that the chosen buffer and any excipients (detergents, proteins) do not interfere with the readout or the compound’s apparent potency.
Item-specific buffer data (pH stability, solubility limits): Not specified for this item; refer to CoA/Spec Sheet and perform pilot tests.
Green Alternatives
Context: As a discrete small-molecule research compound, GSK2647544 itself does not have a “greener substitute.” However, greener choices can be implemented in how the compound is dissolved, handled, and analyzed.
Solvent/process considerations (general):
Prefer water-based assay buffers with minimal DMSO (≤0.5–1% v/v) consistent with assay tolerance.
When organic solvents are necessary, prioritize ethanol or isopropanol over DMF/NMP where chemically and biologically feasible.
For chromatography, adopt water‑rich gradients and modern columns enabling lower organic consumption.
Comparison of common dissolution media (general):
DMSO: High solvency, low volatility; widely accepted in bioassays. Environmental impact moderate; use minimal volumes.
Ethanol: Renewable origin possible; good biocompatibility but limited solvency for highly lipophilic scaffolds.
DMF/NMP: Strong solvency but reproductive toxicity concerns; avoid in biological systems when possible.
Operational green tips:
Aliquot once to reduce repeated thaw/heat cycles that can cause degradation and waste.
Use amber vials and efficient microdosing (acoustic/low‑volume pipetting) to minimize solvent and compound usage.
Consolidate analytical runs and employ UHPLC to reduce solvent volume per sample.
Waste management:
Segregate halogenated vs non‑halogenated organics; capture DMSO-containing aqueous waste per local regulations.
Evaluate potential for solvent recycling in analytical labs.
Pharmaceutical Uses
Regulatory/usage status (Product Data): For research use only. Not for human or veterinary use. No pharmacopeial status is provided for this item.
Appropriate roles in pharmaceutical R&D workflows (non-clinical; general):
Reference standard for analytical method development (LC–MS/MS, HPLC-UV) in discovery ADME or in vitro DMPK studies.
Tool compound for target validation in enzymology and cell biology, supporting mechanism-of-action studies without implying clinical efficacy.
Spiking standard for recovery and stability assessments in bioanalytical matrices (plasma, microsomes, buffer) where permitted.
Formulation screening (discovery scale):
Solubility enhancement strategies may include co-solvent systems (DMSO/EtOH/H2O), pH adjustment if ionizable, or cyclodextrin inclusion—subject to compound chemistry and assay compatibility.
Documentation needs:
Maintain CoA, structural confirmation, and purity data for each lot used in regulated method development or cross-study comparisons.
Limitations:
No claims are made regarding suitability for clinical trials, GMP manufacturing, or therapeutic application. Any such uses would require separate qualification and documentation not supplied with this research-grade item.
Physical Properties
Item-specific values (Product Data):
Appearance: Not specified for this item; refer to CoA/Spec Sheet.
Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.
Commonly requested specifications (this item):
Melting point: Not specified for this item; refer to CoA/Spec Sheet.
Boiling point: Not applicable/rarely defined for complex small-molecule inhibitors; Not specified for this item; refer to CoA/Spec Sheet.
Density: Not specified for this item; refer to CoA/Spec Sheet.
UV-Vis characteristics, HPLC purity UV cutoff, residual solvents, metal limits: Not specified for this item; refer to CoA/Spec Sheet.
LogP/logD, pKa, refractive index: Not specified for this item; refer to CoA/Spec Sheet.
Literature/general expectations for drug-like small molecules (for planning only; verify experimentally):
Many kinase/enzyme-directed small molecules exhibit moderate to high lipophilicity and limited aqueous solubility; DMSO stock solutions (10–50 mM) are commonly prepared.
Solid-state at ambient temperature is typical, with melting points often in the 100–250 °C range; actual value for GSK2647544 must be confirmed from primary sources.
Practical notes:
If solubility screening is required, evaluate DMSO, DMF, ethanol, and aqueous buffers containing co-solvent (e.g., 0.5–2% DMSO or 10–30% acetonitrile), documenting precipitation on dilution.
For photolabile compounds, minimize light exposure (this item requires protection from light per Product Data).
Quality and Grades
Item-specific quality information (Product Data):
Grade/Purity: Not specified for this item; refer to CoA/Spec Sheet.
How to interpret grade/purity (general guidance for small-molecule research reagents):
“Analytical” or “assay” grade typically indicates ≥95% purity by HPLC/UPLC with defined detection wavelengths; may include residual solvent limits.
“Screening” or “library” grade supports HTS/lead discovery; purity often ≥90–95% by HPLC with supporting MS/HRMS identity.
“Reference standard” grade emphasizes identity confirmation (NMR, HRMS) and tight purity specs for quantitation.
Verification steps recommended:
Request and review CoA for this specific lot, including: HPLC/UPLC purity trace, identity confirmation (MS/HRMS, NMR), water/volatile content (KF/LOD), and any stabilizers.
Confirm salt form and polymorph, as these affect solubility and bioassay comparability.
Stabilizers and additives:
Not specified for this item; refer to CoA/Spec Sheet. If none are indicated, assume neat solid and handle under dry, dark conditions.
Fit-for-purpose considerations:
For SAR/HTS: consistency of purity across lots is critical; align detection wavelength with the compound’s chromophores.
For bioanalytical quantitation: obtain a reference lot with full characterization and, if needed, certified potency (assay-corrected content).
Reaction and Applications
This product is a finished small-molecule research compound rather than a synthetic reagent. As such, it is not typically used as a stoichiometric reactant in preparative organic chemistry.
Research applications (non-clinical; literature-based context):
GSK2647544 has been reported in the literature as a selective inhibitor used to interrogate phospholipase A2–related lipid biochemistry in vitro and in cells. When used as a chemical probe, it can help dissect enzyme contribution to lipid mediator generation. Verify the primary references for exact target, potency, and selectivity profile before experimental planning.
Practical usage guidance:
Prepare concentrated DMSO stocks (e.g., 10–50 mM), store aliquoted at −80 °C protected from light, and minimize freeze–thaw cycles.
For cellular assays, conduct a solubility/precipitation check at the intended working concentration and serum level. Include vehicle controls matched for DMSO percentage.
For biochemical assays, confirm enzyme source, substrate, and detection scheme compatibility with the co‑solvent and any excipients.
Analytical applications:
May serve as a reference standard in LC–MS/MS method development for exposure, permeability, or metabolism studies, provided identity/purity are verified for the specific lot.
Note: No synthetic transformation or named-reaction roles are typically applicable to this item.
Reaction Conditions
Not typically applicable: This product is not intended for use as a reagent or catalyst; therefore, standard “reaction conditions” (solvent, temperature, equivalents, catalysts) are not defined for synthetic transformations.
Practical handling conditions for research applications (general):
Stock solution preparation: Dissolve in DMSO to 10–50 mM; vortex and, if needed, brief sonication. Avoid prolonged heating.
Working solutions: Dilute into assay buffer or media with controlled co-solvent (commonly ≤0.1–1% DMSO). Inspect for precipitation or adsorption.
Temperature: Maintain on ice or at 2–8 °C while preparing dilutions; return aliquots to −80 °C promptly. Avoid repeated freeze–thaw.
Light sensitivity: Handle under low light; use amber tubes/plates consistent with the Product Data requirement to protect from light.
Stability testing suggestions (if critical to your workflow):
Assess bench-top, refrigerated, and 37 °C stability in the intended matrix (buffer, media, plasma) by LC–MS at relevant time points.
Include control experiments for adsorption to plastics and recovery after filtration.
Item-specific kinetic/thermodynamic data: Not specified for this item; refer to CoA/Spec Sheet and primary literature.
Safety and Handling
GHS/CLP classification (Product Data):
Signal word: Not specified for this item; refer to SDS.
Hazard statements (H-phrases): Not specified for this item; refer to SDS.
Pictograms: Not specified for this item; refer to SDS.
General laboratory precautions (best practice for research-only small molecules):
Use in a chemical fume hood; avoid inhalation, ingestion, and skin/eye contact.
Wear appropriate PPE: lab coat, safety glasses, and suitable gloves (nitrile recommended). For weighed powders, consider dust mask or respirator per risk assessment.
Prevent environmental release; collect waste in halogenated or non‑halogenated organic waste streams as appropriate.
Handling notes specific to this listing:
Protect from light and maintain cold chain integrity; the item is shipped on dry ice/cold packs and should be kept at −80 °C upon receipt.
Allow vials to equilibrate to room temperature in a desiccated, dark environment before opening to minimize condensation.
Incompatibilities and stability (general):
Avoid strong oxidizers and strong acids/bases unless stability is known.
Sensitive small molecules may degrade with moisture, heat, or prolonged light exposure; use amber vials and low‑light handling.
First aid (summary; defer to SDS for authoritative guidance):
Skin/eye contact: Rinse with water for at least 15 minutes; remove contaminated clothing; seek medical advice.
Inhalation: Move to fresh air; seek medical attention if symptoms persist.
Ingestion: Rinse mouth; do not induce vomiting; seek medical attention.
Regulatory note: For research use only; not for human or veterinary use.
Solvent Selection
Item-specific solubility data: Not specified for this item; refer to CoA/Spec Sheet.
General selection strategy for drug-like heteroaromatic small molecules:
Primary stock solvent: DMSO is typically preferred due to broad solvating power and compatibility with biochemical assays.
Alternative strong dipolar aprotic solvents: DMF or NMP can be used for initial dissolution, followed by dilution into assay buffer with controlled co‑solvent levels.
Protic/organic cosolvents: Ethanol or isopropanol may aid dissolution for less polar solids; confirm assay tolerance.
Aqueous work:
For buffers, pre‑dissolve in DMSO to a concentrated stock (e.g., 10–50 mM), then dilute into buffer ensuring final DMSO ≤0.1–1% v/v or per assay limit to avoid precipitation.
Employ surfactants (e.g., 0.01–0.05% Tween‑80) cautiously if permitted by the assay to reduce aggregation and adsorption.
Comparative considerations:
DMSO vs DMF: DMSO is less volatile and more biocompatible in assays; DMF may offer marginally better solubility for certain scaffolds but can impact enzyme activity.
Aqueous cosolvent strategies: ACN/H2O (10–30% ACN) for chromatography; avoid high ACN in enzyme assays unless validated.
Practical tips:
Warm gently (25–40 °C) and vortex/sonicate to aid dissolution; avoid prolonged heating.
Filter 0.22 µm if particulate persists; beware of analyte adsorption to nylon—use PTFE or PVDF filters.
Storage and Reconstitution
Storage conditions (from Product Data):
Store at −80 °C.
Protect from light.
Shipped on dry ice packs + cold packs. Maintain cold chain on receipt.
Reconstitution (item-specific details): Not specified for this item; refer to CoA/Spec Sheet.
General reconstitution guidance for small-molecule solids:
Allow vial to warm in a desiccated, dark environment to avoid condensation before opening.
Prepare a concentrated stock in an anhydrous, compatible solvent—commonly DMSO (e.g., 10–50 mM). Vortex and, if needed, sonicate briefly. Do not heat excessively.
If particulate persists, consider gentle warming (≤40 °C) and sterile filtration using PTFE/PVDF 0.22 µm filters if sterility is required by the assay.
Aliquoting and stability:
Dispense single-use aliquots to minimize freeze–thaw. Store aliquots at −80 °C in amber vials or foil-wrapped tubes.
Record preparation date and calculated concentration; monitor for precipitation or color change upon thawing/dilution.
In-use handling:
Keep working solutions on ice or at 2–8 °C and shielded from light during assay setup. Discard any remaining diluted solutions after the experiment unless stability is validated.
Expiry:
If an expiration or retest date is required, consult the CoA/Spec Sheet or establish an internal retest period based on stability studies under your storage conditions.
Structure and Identity
Item-specific identifiers (from Product Data):
SKU: G646149
Product Name: GSK2647544
CAS: 1380426-95-8
PubChem CID: 57336782
InChIKey: Not specified for this item; refer to CoA/Spec Sheet.
SMILES: Not specified for this item; refer to CoA/Spec Sheet.
Molecular formula: Not specified for this item; refer to CoA/Spec Sheet.
Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.
Structural features (general description; literature):
GSK2647544 is reported in the literature as a drug-like, heteroatom-containing small molecule designed for enzyme inhibition. Full 2D atom connectivity, stereochemistry (if any), and functional-group annotation should be confirmed from the primary reference or PubChem (CID above).
Typical features for this class include multiple aromatic/heteroaromatic motifs and polar heteroatoms (e.g., N/O) arranged to engage catalytic/affinity pockets. Exact ring systems and stereocenters must be verified from the structure record.
2D structure in words (how to read once structure is at hand; general guidance):
Identify core scaffold (e.g., biaryl, azaheteroaryl, or fused ring) and map substituents by position numbers.
Note H-bond donor/acceptor sites, cation/anion centers (if ionizable), and lipophilic regions; these features rationalize solubility and binding.
Provenance reminder:
Where exact structure descriptors are required for registration or computational use, retrieve them directly from the certificate/specification or the cited database entry to avoid transcription errors.
Synthetic Utility
Role in synthesis: GSK2647544 is an end-product small-molecule inhibitor and is not generally employed as a synthetic building block or reagent. It lacks broadly useful functional handles intended for downstream diversification under routine conditions.
When it can be useful synthetically (niche scenarios):
As an analytical reference to benchmark synthetic intermediates or analogs in SAR programs (e.g., retention time matching, MS/NMR comparison).
As a positive control to validate target engagement assays when exploring alternative synthetic routes to related chemotypes.
Alternative strategies for derivative preparation (general):
If the scaffold is desired for analoging, de novo synthesis from published routes is recommended rather than derivatization of the final inhibitor, which could be structurally complex and sensitive to modifications.
Conclusion:
For most laboratories, this compound should be treated as a tool molecule/reference standard rather than a reagent for bond-forming transformations.
Target Specificity
Item-specific target data from Product Data: Not specified for this item; refer to CoA/Spec Sheet.
No antigen/epitope/clone/isotype information is applicable, as this is a small-molecule compound, not an antibody or biologic.
Literature note (context only; verify with original sources before use):
GSK2647544 has been described as a selective small-molecule inhibitor for a phospholipase A2–related enzymatic target. Exact target identity, species cross-reactivity, and selectivity panel should be confirmed from peer-reviewed publications and database records associated with the CAS and CID provided.
Recommendation:
For rigorous studies, document the target, IC50/Ki, and selectivity metrics for your lot and assay conditions, and include appropriate orthogonal assays to exclude off-target effects.
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