EPZ015666 - Moligand™, ≥98%(HPLC) , Inhibitor of protein arginine methyltransferase 5, CAS No.1616391-65-1, Inhibitor of protein arginine methyltransferase 5
EPZ015666 - Moligand™, ≥98%(HPLC) , Inhibitor of protein arginine methyltransferase 5, CAS No.1616391-65-1, Inhibitor of protein arginine methyltransferase 5
GRAU & PUREZAMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.≥98%(HPLC)
Inibidor seletivo e potente (IC 50 = 22nM, K i =5 nM) da arginina metiltransferase 5 (PRMT5). Apresenta seletividade para a PRMT5 em relação a um painel de 20 outras proteínas metiltransferases.
This compound belongs to the class of organic compounds known as tetrahydroisoquinolines. These are tetrahydrogenated isoquinoline derivatives.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
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Application Protocols
Product Data (item-specific): No tested applications or recommended dilutions are specified for this item.
General, literature-informed starting points (not item-specific; validate locally)
Biochemical enzyme assay: Prepare a 10 mM DMSO stock. Perform serial dilutions to cover a broad concentration range. Maintain constant vehicle concentration and include controls (no-inhibitor, vehicle-only, known reference inhibitor if available).
Cell-based assay: Dose cells with a dilution series (e.g., 0.01–10 μM as a broad screen), monitor viability and pathway biomarkers (e.g., SDMA levels by immunoblot). Optimize exposure time (e.g., 24–96 h) per cell model.
Target engagement: Use thermal shift or CETSA with appropriate protein detection to confirm on-target interaction under assay conditions.
These are generic guidelines from the literature for chemical probes of this class and are not performance specifications for this item.
EPZ015666 is reported in the literature as a selective, potent inhibitor of protein arginine methyltransferase 5 (PRMT5), commonly used as a chemical probe to study symmetric arginine dimethylation on histones and non-histone substrates. Through PRMT5 modulation, researchers interrogate roles in transcriptional regulation, RNA splicing, and chromatin architecture.
Typical experimental readouts include changes in symmetric dimethyl-arginine (SDMA) marks by immunoblotting, alterations in gene expression (RNA-seq/qPCR), and functional phenotypes in cellular models.
Selectivity profiling in publications often covers panels of PRMT family members and broader epigenetic enzymes to contextualize off-target risks; users should consult the primary data to align dose/exposure with intended selectivity windows.
Best practices for biological studies
Use concentration ranges that bracket reported biochemical/cellular potencies and include orthogonal probes or inactive analogs where available for target-validation controls (literature practice).
Confirm target engagement in the specific biological system (e.g., CETSA, NanoBRET, occupancy assays) rather than relying solely on historical potency figures.
Consider time-dependency and protein turnover; sustained exposure may be required to observe downstream biomarker changes.
Note: All uses are for research only. No clinical or diagnostic applications are implied.
Buffer Applications
This compound is not a buffer reagent. However, buffers are central to its use in biochemical assays.
Practical guidance (general)
Enzymology assays: Use standard assay buffers (e.g., HEPES/Tris at pH 7–8), including required cofactors and salts for methyltransferase activity, ensuring the final DMSO percentage is constant across conditions.
Protein binding/thermal shift: Employ low-detergent buffers (e.g., HEPES with 100–300 mM NaCl) to reduce nonspecific aggregation; include reducing agents only if compatible with the protein target.
Cell-based assays: Use complete culture media; maintain a stable vehicle concentration and pre-equilibrate compound in media to reduce precipitation. Consider serum effects on free fraction.
Tips
Filter buffers (0.22 μm) for cell-based work and degas for sensitive biophysical assays.
Validate that buffer components do not chemically react with the compound or affect readouts (fluorescence, absorbance, luminescence).
Green Alternatives
Green chemistry comparisons are generally not applicable to this product because it functions as a bioactive probe rather than as a solvent or process reagent.
Considerations (general)
If large volumes of DMSO are used for high-throughput screening, minimize solvent consumption by employing miniaturized assay formats (e.g., 384/1536-well plates) and acoustic dispensing to reduce waste.
Implement solvent recycling where feasible and ensure proper waste segregation for DMSO-containing aqueous streams.
Choose aqueous assay buffers and low organic cosolvent percentages when compatible with compound solubility and assay performance.
Alternative practices
Where possible, utilize green-compatible assay detection technologies (e.g., label-free or low-toxicity readouts) to reduce hazardous reagent use.
Adopt right-first-time experimental design (DoE) to limit repeat runs and associated solvent/consumable use.
Pharmaceutical Uses
No pharmaceutical or therapeutic uses are claimed for this catalog item. It is supplied strictly for research use only.
General formulation context (literature/general; not item-specific)
Bioactive probes like EPZ015666 are sometimes formulated for in vivo research using vehicles such as aqueous solutions with cosolvents/surfactants (e.g., DMSO/PEG/saline combinations) when allowed by institutional protocols. Any such use must be supported by primary literature and IACUC approvals.
For in vitro ADME profiling, standard panels include microsomal stability, plasma protein binding, and permeability assays; solvent carryover should be minimized to avoid assay artifacts.
Compliance
Not intended for human or veterinary use. No pharmacopeial monograph is implied. Users are responsible for regulatory compliance in their jurisdiction.
Physical Properties
Product Data (item-specific)
Appearance: Not specified for this item; refer to CoA/Spec Sheet.
Molecular Weight: Not specified for this item; refer to CoA/Spec Sheet.
Molecular Formula: Not specified for this item; refer to CoA/Spec Sheet.
Literature/general properties for EPZ015666 (not item-specific; verify against primary references before use)
State/form: Typically supplied as a solid bioactive small molecule for screening libraries.
Solubility (assay practice): Commonly prepared as a concentrated DMSO stock (e.g., 10–50 mM) for biochemical or cell-based assays; further diluted into aqueous assay buffers containing carrier solvent (literature).
Aqueous behavior: Like many hydrophobic probes, direct water solubility is limited; use cosolvent and/or surfactant (e.g., 0.1–1% DMSO or nonionic detergent) as compatible with the assay system (literature).
LogP, pKa, BP/MP, density, refractive index: Not specified here; consult primary databases or computational predictions as needed for method development.
Practical notes (general)
Filter sterilization of working solutions (0.22 μm) may be performed for cell-based assays if chemically compatible.
Avoid repeated freeze–thaw of concentrated DMSO stocks to minimize precipitation and potency drift.
Light/moisture sensitivity can vary by scaffold; protect from light and air when feasible until item-specific data are available.
Quality and Grades
Product Data (item-specific)
Grade/Purity: Moligand™
What Moligand™ implies (general description of grade; not item-specific specifications)
Moligand™ denotes a research-grade small-molecule ligand suitable for discovery biology, screening, and mechanistic studies. Emphasis is typically placed on identity confirmation and suitability for biochemical/cellular assays rather than chromatographic solvent specifications.
Typical expectations for this grade include: confirmed identity (e.g., by NMR/HRMS/HPLC) and assay-appropriate purity. Exact analytical acceptance criteria for this specific lot are Not specified for this item; refer to CoA/Spec Sheet.
Practical considerations
For quantitative biology (e.g., IC50/Ki determinations), request and review the CoA for purity, residual solvent content, and analytical method details.
For orthogonal confirmation, users may perform in-house QC (e.g., LC–MS purity check under assay-relevant gradients) to ensure matrix compatibility and low UV background if optical readouts are used.
If stabilizers or salt forms are applied, they will be listed on the CoA; no stabilizer information is provided in the Product Data.
Reaction and Applications
This item is supplied as a bioactive screening ligand and is not typically used as a stoichiometric reagent, catalyst, solvent, or building block in synthetic chemistry.
Research application context (literature/general)
EPZ015666 is widely used in discovery biology as a chemical probe in biochemical assays, cell-based studies, and target-engagement experiments to interrogate arginine methyltransferase pathways (literature). Applications include potency ranking, time-dependent inhibition assessments, and combination studies with orthogonal epigenetic modulators.
Common assay modalities: radiometric methyltransferase assays, fluorescence/luminescence readouts, CETSA/thermal shift for target engagement, and transcriptomic/proteomic downstream analyses.
Practical usage tips (general)
Prepare fresh working solutions from concentrated DMSO stocks immediately before assays to minimize adsorption losses and potential degradation.
Include a vehicle control matching the highest DMSO content in test wells.
For kinetic or washout studies, confirm compound stability in the full assay matrix and across the intended time window (pre-incubation vs. co-incubation protocols).
For synthetic transformations or named reactions, this compound is not generally applicable; refer instead to “Biological Roles,” “Application Protocols,” and “Storage & Reconstitution” for guidance relevant to its use as a chemical probe.
Reaction Conditions
As a bioactive probe, this compound is not used as a reagent in chemical reactions; therefore, synthetic reaction conditions are not applicable.
Assay condition guidance (literature/general)
Stock solutions: Often prepared at 10–50 mM in anhydrous DMSO, stored cold and protected from light; diluted into assay buffer immediately before use.
Biochemical assays: Enzyme concentrations, substrate levels, and SAM cofactor concentrations should be optimized empirically. Maintain constant vehicle (DMSO) across wells and include appropriate positive/negative controls.
Cell-based assays: Titrate across logarithmic concentration series (e.g., 8–10 points) with sufficient incubation time to capture downstream biomarker responses; verify compound stability in full media over the assay duration.
Expected outcomes
Potency and efficacy values (IC50/EC50) are system-dependent; consult primary literature for ranges reported for EPZ015666 in the specific assay context. No item-specific performance specifications are provided here.
Safety and Handling
Product Data (item-specific)
GHS Classification: Not specified for this item; refer to SDS.
Signal Word: Not specified for this item; refer to SDS.
Hazard (H) Statements: Not specified for this item; refer to SDS.
Pictograms: Not specified for this item; refer to SDS.
Storage Conditions: Store at -20°C
Shipped In: Ice chest + Ice pads
General laboratory precautions (not item-specific; follow institutional EHS policies and the SDS)
PPE: Use lab coat, safety glasses, and appropriate chemically resistant gloves. Handle powders/solids in a fume hood or ventilated enclosure to minimize dust/aerosol exposure.
Incompatibilities: Avoid strong oxidizers and strong acids/bases unless compatibility is verified. Keep away from ignition sources when using organic solvents (e.g., DMSO, DMF, ethanol) as vehicles.
First aid (overview): In case of skin/eye contact, rinse with water for at least 15 minutes; remove contaminated clothing. If inhaled, move to fresh air. If ingested or on significant exposure, seek medical attention. Always consult the SDS for authoritative guidance.
Environmental: Prevent release to drains where prohibited; dispose via approved chemical waste streams.
Special risks: As a potent bioactive small molecule, minimize exposure and cross-contamination. Use dedicated tools and secondary containment for weighing and solution prep. Defer to the product’s SDS for all hazard classifications and exposure controls.
Solvent Selection
This product is a bioactive small molecule typically used as a chemical probe rather than as a solvent or reaction medium.
Primary stock solvent: Anhydrous DMSO is commonly used to prepare 10–50 mM master stocks due to broad solubilizing power and assay compatibility.
Working solutions: Dilute into aqueous buffers or culture media to the desired final concentration, maintaining a low final DMSO fraction (often ≤0.1–0.5% v/v) consistent with biological system tolerance.
Alternative vehicles: DMF or ethanol may solubilize some scaffolds; confirm cell/assay compatibility and compound stability before routine use.
Compatibility tips
Pre-warm and vortex during dilution to minimize precipitation; if needed, include a brief sonication.
Use polypropylene labware for DMSO stocks; glass is preferred for long-term storage to minimize leaching.
Filter sterilize only if the compound is known to be stable to the filter polymer and process.
When to choose alternatives
If precipitation occurs at target working concentrations, consider cosolvent strategies (DMSO + aqueous buffer with serum or mild nonionic surfactant) or reduce final dosing concentration while maintaining assay sensitivity.
Storage and Reconstitution
Product Data (item-specific)
Storage Conditions: Store at -20°C
Shipped In: Ice chest + Ice pads
Item-specific details not provided
Appearance, exact solvent recommendations, and concentration limits: Not specified for this item; refer to CoA/Spec Sheet.
General guidance for bioactive small molecules (not item-specific)
Reconstitution: Dissolve the solid in anhydrous DMSO to prepare a concentrated master stock (e.g., 10–50 mM). Mix thoroughly (vortex/brief sonication) until fully dissolved.
Aliquoting: Split master stocks into single-use aliquots (e.g., 10–50 μL) in solvent-compatible vials or tubes to avoid repeated freeze–thaw cycles.
Storage of solutions: Store aliquots at -20°C or below, protected from light and moisture. Minimize headspace to reduce oxidative degradation; consider inert gas overlay for long-term storage.
Thawing/handling: Thaw quickly at room temperature, use immediately, and refreeze remaining aliquots promptly once. Discard aliquots showing precipitation, discoloration, or unexpected LC–MS profiles.
Aqueous working solutions: Prepare immediately before use; if stability permits, hold on ice and use within the same day. Validate stability in your specific buffer/media.
Always consult the product’s CoA and SDS for authoritative, lot-specific instructions.
Structure and Identity
Overview: EPZ015666 is a cataloged bioactive small molecule supplied for research use (SKU: E167694). Item-level structural identifiers are limited in the Product Data; consult the CoA/Spec Sheet for definitive identity attributes.
Product Data (item-specific)
SKU: E167694
Product Name: EPZ015666
CAS: 1616391-65-1
PubChem CID: 90241673
InChIKey: 459827 (as provided)
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.
Literature/general notes (not item-specific)
EPZ015666 is widely described in the literature as a selective chemical probe for protein arginine methyltransferase 5 (PRMT5). Cite primary literature/compound databases for definitive structural depictions.
Typical small-molecule features reported for this scaffold include polycyclic aromatic/heteroaromatic motifs and H-bond acceptor/donor sites consistent with enzyme binding. Exact 2D structure, stereochemistry, and tautomeric form should be verified against primary references.
2D structure description (general/literature)
Reported structures depict a rigid aromatic core with heteroatoms capable of forming key interactions in the SAM-binding vicinity of PRMT5. Without item-level SMILES, a precise atom-by-atom description is not provided here; please refer to authoritative databases (literature).
Synthetic Utility
This product is not typically employed as a synthetic reagent, intermediate, or building block.
General guidance
If structural modification or SAR exploration is of interest, medicinal chemistry teams usually synthesize analogs de novo rather than derivatizing a finished probe substance, due to IP, purity, and route-efficiency considerations.
For analytical method development (not a transformation), the compound may serve as a reference standard in LC–MS or HPLC assays to benchmark retention behavior and establish stability-indicating methods.
Alternative sections
For practical usage, see “Biological Roles,” “Application Protocols,” and “Storage & Reconstitution.”
Target Specificity
Product Data (item-specific): Not specified for this item; refer to CoA/Spec Sheet.
Note
While EPZ015666 is described in literature as a PRMT5 inhibitor, Aladdin provides no item-specific target certification in the Product Data above. Users should consult primary literature and perform local target-engagement controls as appropriate.
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