CBP/p300-IN-1 - Moligand™, 10 mM in DMSO , CAS No.2443789-32-8

CAS: 2443789-32-8 Cat. No.: C1494490 Formula: C₂₃H₂₃FN₂O₅ Peso molecolare: 426.4

GRADE & PURITY Moligand™, 10 mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor.

Specifications

Specifiche e purezza

Moligand™, 10 mM in DMSO

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Grado

Moligand™

Tipo di azione

INHIBITOR

Nomi e identificatori

Peso molecolare

426.4

Reaxy-Rn

40986238

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=40986238&ln=

Application Protocols

Tested applications and recommended conditions are not provided in the current product data.

General handling guidance (non-validated, for planning only):

• Stock preparation: Dissolve in anhydrous DMSO to make a concentrated stock (e.g., 10–50 mM), vortex and sonicate briefly if needed. Verify complete dissolution visually and by analytical means if critical.
• Working solutions: Dilute into assay buffer immediately prior to use; maintain a consistent vehicle concentration across controls and treatments.
• Controls: Include vehicle-only controls and, where available, orthogonal CBP/p300 probes for benchmarking. Determine assay windows and citability via your validated SOPs.

For validated, product-specific protocols and activity data, consult the CoA/Spec Sheet or contact Technical Support.

Biological Roles

Context (general biology; not item-specific claims):

• CBP (CREB-binding protein) and p300 (EP300) are paralogous transcriptional coactivators possessing intrinsic lysine acetyltransferase (KAT/HAT) activity and reader modules (e.g., bromodomains) that recognize acetyl-lysine marks. They integrate multiple signaling pathways, bridging transcription factors to the transcriptional machinery and chromatin.
• Enzymology: The KAT domains acetylate histones (e.g., H3K27, H3K18) and numerous non-histone substrates, modulating chromatin accessibility and protein–protein interactions. Bromodomains bind acetylated lysines, contributing to chromatin targeting and complex assembly.
• Functional impact: CBP/p300 regulate gene expression programs in development, differentiation, and stress responses. Dysregulation by mutation, altered expression, or aberrant recruitment can perturb global acetylation patterns and transcriptional output.
• Chemical probes: Small-molecule inhibitors have been developed to modulate either the bromodomain or the KAT catalytic site. Such probes enable dissection of CBP/p300-dependent transcription, acetylation dynamics, and enhancer activity in cells and biochemical systems.

Use of CBP/p300-IN-1 (general intent):

• As a research ligand putatively targeting CBP/p300, compounds in this class are utilized to interrogate target engagement, selectivity versus related bromodomains or KATs, and downstream transcriptional consequences. Item-specific potency, selectivity, and binding mode are Not specified for this item; refer to CoA/Spec Sheet and primary literature linked to the CAS/CID if required.

Buffer Applications

This listing is a small-molecule ligand rather than a buffering agent. It does not serve as a pH buffer component.

Practical note (general for assay prep):

• Prepare working solutions by diluting DMSO stocks into your assay buffer of choice (e.g., HEPES, Tris, or PBS-based systems), maintaining low vehicle percentages. Specific buffer recipes or pH ranges are application-dependent and not specified for this item.

Green Alternatives

Green chemistry substitution analysis is generally applicable to solvents and bulk reagents. For a discrete screening ligand such as CBP/p300-IN-1, the concept of a “green alternative” is not typically relevant.

Considerations (general):

• If your concern is reducing hazardous solvent use during dissolution, prioritize DMSO over chlorinated solvents, and employ minimal solvent volumes with aqueous buffers where compatible.
• For assay platforms, reduce plastic waste by adopting miniaturized formats and reusable labware where possible.

For process-scale needs or if you seek greener probe chemotypes with similar biological profiles, review the literature for CBP/p300 tool compounds with improved stability/solubility profiles; however, such choices are driven by biological selectivity and ADME, not classical green metrics.

Pharmaceutical Uses

This product is supplied strictly for research use only and is not approved for human or veterinary use. No pharmacopeial status or excipient role is provided for this item.

Context (general information):

• Small-molecule CBP/p300 ligands are commonly used in discovery research to explore target biology, structure–activity relationships (SAR), and assay development. Any discussion of therapeutic application is beyond the scope of this catalog entry and is not implied by the product’s availability.

Item-specific formulation/manufacturing details: Not specified for this item; refer to CoA/Spec Sheet.

Physical Properties

Item-specific physicochemical data are not provided in the current listing.

• 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/unknown for a discrete solid screening ligand; refer to CoA/Spec Sheet if available.
• Density: Not specified for this item; refer to CoA/Spec Sheet.
• Solubility: Not specified for this item; refer to CoA/Spec Sheet. (General practice for small-molecule inhibitors: prepare DMSO stock and dilute into assay buffer with ≤1% DMSO final.)
• 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/UV cutoff: Not specified for this item; refer to CoA/Spec Sheet.

Guidance (general literature/practice, not item-specific):

• Many CBP/p300 modulators are moderately lipophilic and formulated as 10–50 mM DMSO stocks for biochemical or cell-based assays. Actual solubility and stability should be verified experimentally for this specific lot.

Quality and Grades

• Grade/Purity: Moligand™

Context for this item:

• Moligand™ denotes a research-grade small-molecule ligand suitable for discovery screening, target validation, and mechanism studies. It emphasizes identity confirmation and fitness for biochemical/cellular assay use rather than process-scale or GMP compliance.

What Moligand™ typically implies (general guidance):

• Suitability for generating DMSO stocks for HTS, fragment-to-lead exploration, or chemical biology probing.
• Batch documentation available on request (e.g., CoA) with core identity data (NMR/LC–MS/HPLC). Specific numeric specifications such as purity percentage, water content, metal limits, and residual solvent levels are Not specified for this item; refer to CoA/Spec Sheet.
• Not intended for human or veterinary use; For research use only.

Stabilizers/additives:

• Not specified for this item; refer to CoA/Spec Sheet.

When to choose this grade:

• Early-stage SAR, phenotypic screens, target engagement assays, or tool-compound controls in epigenetics programs focused on CBP/p300. For regulated manufacturing or in vivo enabling studies requiring tightly defined impurity profiles, request enhanced documentation or alternative grades if available.

Reaction and Applications

This product is supplied as a research ligand/inhibitor for biological studies and compound screening, not as a synthetic reagent or solvent. Consequently, it is not typically employed in named organic reactions or as a stoichiometric/catalytic reagent.

Where it is relevant (general application context):

• Chemical biology and epigenetics research as a probe for CBP/p300-related pathways in biochemical assays (e.g., HAT or bromodomain binding assays) and cell-based target engagement. Specific application details for this catalog item are not provided here; consult primary literature on CBP/p300 chemical probes and your assay SOPs.

If you require a synthetic intermediate or functionalized analog for SAR or conjugation, please contact us with your needs; the current listing does not specify such utility.

Reaction Conditions

Not applicable. This product is not intended for use as a reagent or catalyst in synthetic chemistry. No reaction conditions are specified for this item.

For biological assays (general practice, not item-specific):

• Biochemical assays targeting CBP/p300 are commonly conducted at ambient temperature in buffered aqueous media containing low DMSO. Kinetic or endpoint readouts (e.g., TR-FRET, Alpha, HTRF, enzyme-coupled acetylation assays) are platform-specific and beyond the scope of this listing.

Safety and Handling

• GHS classification: Not specified for this item; refer to SDS.
• Signal word/H-statements/Pictograms: Not specified for this item; refer to SDS.

General laboratory safety (professional guidance):

• Handle in a chemical fume hood, using standard PPE: lab coat, safety glasses, and appropriate chemically resistant gloves (e.g., nitrile). Avoid inhalation of dust/aerosols and skin/eye contact.
• Avoid repeated freeze–thaw of DMSO stocks to minimize potential decomposition or precipitation.
• Incompatibilities: Until specific data are available, avoid strong oxidizers and strong acids/bases. Keep away from moisture if supplied as a dry solid.
• First aid (overview; defer to SDS):
  • Inhalation: Move to fresh air; seek medical attention if symptoms persist.
  • Skin/eye contact: Rinse with plenty of water for at least 15 minutes; remove contaminated clothing; seek medical attention if irritation persists.
  • Ingestion: Rinse mouth; do not induce vomiting; seek medical attention.
• Spill response: Avoid dust generation; absorb solutions with inert material; collect in compatible waste.
• Waste disposal: Dispose of as organic laboratory chemical waste according to institutional and local regulations.

Authoritative source: Always consult the product’s Safety Data Sheet (SDS) and your institutional EHS guidance for hazard classification and detailed handling procedures.

Solvent Selection

This product is a small-molecule inhibitor intended for biochemical/cell-based assays rather than as a bulk solvent.

Practical dissolution guidance (general, not item-specific):

• Primary solvent: DMSO is typically preferred for hydrophobic inhibitors. Start with 10–50 mM stock concentration; adjust based on observed solubility and stability.
• Aqueous use: Dilute DMSO stock into assay buffer (e.g., HEPES- or Tris-based, with 0.01–0.1% nonionic surfactant if needed) maintaining ≤0.5–1% DMSO final to minimize vehicle effects in cells/enzymes.
• Co-solvent alternatives: If DMSO is unsuitable, consider DMF or ethanol for primary dissolution, then immediate dilution into buffer. Verify compatibility with assay components.
• Filtration: If particulates persist, sterile-filter (0.22 µm PTFE/nylon) post-dilution; avoid adsorptive losses by pre-wetting filters with vehicle.

Comparison (general literature tendencies for CBP/p300 ligands):

• DMSO: Best balance of solubilizing power and biocompatibility at low percentages.
• DMF: Similar solubilizing power; greater cytotoxicity risk; limit final %.
• Ethanol: May be acceptable at ≤0.5% v/v but can perturb membrane/cellular responses.

Always determine actual solubility, stability, and assay interference for this specific item experimentally. Consult the CoA/Spec Sheet for any item-specific solvent recommendations if provided.

Storage and Reconstitution

• Storage conditions (item-specific): Store at -80°C.
• Shipped in (item-specific): Dry ice packs + Cold packs.
• Research use note: For research use only.

Stability and handling (general guidance, not item-specific specifications):

• Upon receipt, keep frozen at -80°C. If supplied as a solid, allow the container to equilibrate to room temperature in a desiccator before opening to prevent condensation. If supplied as a solution, keep frozen and minimize time at ambient temperature.
• Aliquoting: Prepare single-use aliquots of DMSO stock to avoid repeated freeze–thaw cycles. Typical working stocks are maintained at -20 to -80°C in tightly sealed, low-bind vials.
• Light/moisture: Protect from light and moisture until use unless the CoA indicates otherwise.
• Reconstitution: Not specified for this item; refer to CoA/Spec Sheet. General practice is to dissolve in anhydrous DMSO, verify clarity, and filter if particulate persists after dilution.

Always consult the CoA/Spec Sheet for any lot-specific stability data, recommended stock concentration limits, and confirmed solvent compatibility.

Structure and Identity

• Product name: CBP/p300-IN-1 (SKU: C1494490)
• CAS: 2443789-32-8
• CID: 137628649
• Molecular formula: Not specified for this item; refer to CoA/Spec Sheet.
• Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.
• InChIKey: Not specified for this item; refer to CoA/Spec Sheet.
• SMILES: Not specified for this item; refer to CoA/Spec Sheet.
• Structural features (general): This listing denotes a small-molecule inhibitor targeting the bromodomain/acetyltransferase coactivators CBP/p300. Specific functional groups, ring systems, or stereochemistry are not disclosed in the current product data.
• 2D structure description: Not specified for this item; refer to CoA/Spec Sheet.

Notes:

• Item-specific identifiers beyond CAS/CID are not provided here. Please consult the accompanying CoA/Spec Sheet for definitive structural identifiers suitable for registration or ELN documentation.

Synthetic Utility

Not typically applicable. CBP/p300-IN-1 is offered as a finalized research ligand/probe, not as a synthetic building block.

If you plan to derivatize or immobilize the compound (e.g., for chemoproteomics or pull-down assays), please consult the structural data and functional group availability in the CoA/Spec Sheet. At present, functional handles, protecting-group status, and reactivity are Not specified for this item.

Target Specificity

Only product-data-supported information may be listed here.

• Intended class: Small-molecule ligand associated with CBP/p300 research (general).
• Specific target isoforms/subdomains (e.g., bromodomain vs KAT), Ki/IC50, and selectivity panels: Not specified for this item; refer to CoA/Spec Sheet and primary literature corresponding to CAS 2443789-32-8 / CID 137628649.

No antibody/biologic attributes (epitope, clone, isotype) apply to this small-molecule product.