| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
TRRAP-IN-1 targets the protein-protein interaction between MYC and TRRAP (Transformation/Transcription Domain-Associated Protein). TRRAP is a component of multiple histone acetyltransferase complexes and is recruited by MYC to activate transcription of target genes involved in cell proliferation and metabolism. By inhibiting this interaction, TRRAP-IN-1 disrupts MYC-mediated transcriptional activation.
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| ln Vitro |
In vitro activity of TRRAP-IN-1 has been evaluated in cell-based assays measuring its ability to inhibit MYC:TRRAP interaction and suppress MYC-driven transcription. While specific IC₅₀ values for the interaction inhibition are not extensively reported in the available literature, the compound has been validated as a potent disruptor of this protein-protein interaction in biochemical and cellular contexts.
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| ln Vivo |
In vivo activity of TRRAP-IN-1 has been investigated in anti-tumor research models. As an inhibitor of the MYC:TRRAP interaction, the compound shows potential for suppressing tumor growth in MYC-dependent cancers. Preclinical studies have demonstrated the importance of this interaction in tumor maintenance, and pharmacological inhibition represents a promising therapeutic strategy.
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| Enzyme Assay |
Non-cell-based binding assays for TRRAP-IN-1 typically involve surface plasmon resonance (SPR) or fluorescence polarization (FP) to measure the inhibition of MYC:TRRAP protein-protein interaction. A typical protocol includes: immobilizing TRRAP protein on a sensor chip, flowing MYC protein with varying concentrations of the compound, and calculating binding affinity (Kd) or inhibition potency (IC₅₀) from the response data.
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| Cell Assay |
Cellular assays for TRRAP-IN-1 typically involve MYC-dependent cancer cell lines. A representative protocol includes: culturing cells in appropriate medium, treating with TRRAP-IN-1 at various concentrations (0.1–50 μM) for 24–72 hours, and assessing cell viability using MTT or CellTiter-Glo assays. MYC target gene expression can be measured by qRT-PCR or Western blot to confirm on-target activity.
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| Animal Protocol |
In vivo animal studies with TRRAP-IN-1 typically involve xenograft mouse models of MYC-driven tumors. A representative protocol includes: subcutaneous implantation of tumor cells in immunodeficient mice, allowing tumors to reach a certain size, administering TRRAP-IN-1 via oral gavage or intraperitoneal injection at doses determined from pharmacokinetic studies, monitoring tumor growth and body weight, and harvesting tumors for histopathological and molecular analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TRRAP-IN-1 have not been extensively reported in the available literature. As a small molecule inhibitor of protein-protein interactions, it is expected to have moderate oral bioavailability and tissue distribution. Further PK studies are needed to characterize its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
Toxicological data for TRRAP-IN-1 are limited as the compound is in preclinical research stages. Standard safety assessments would include cytotoxicity screening, hERG channel inhibition testing, and preliminary toxicology studies in animal models. As a research compound, it is not intended for human therapeutic use.
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| References | |
| Additional Infomation |
TRRAP-IN-1 (CAS 857254-94-5) represents a novel class of MYC:TRRAP interaction inhibitors with potential applications in oncology research. The compound is also referred to as (6aR,11aR)-6a,11a-dihydro-4-(3-methyl-2-buten-1-yl)-6H-benzofuro[3,2-c][1]benzopyran-3,9-diol. It is typically stored under recommended conditions as specified in the certificate of analysis.
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| Molecular Formula |
C20H20O4
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|---|---|
| Molecular Weight |
324.370406150818
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| CAS # |
857254-94-5
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| Appearance |
Typically exists as solid at room temperature
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| SMILES |
C1OC2=C(C/C=C(/C)\C)C(O)=CC=C2[C@]2([H])OC3=CC(O)=CC=C3[C@]12[H]
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Typically soluble in DMSO (e.g. 10 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0829 mL | 15.4145 mL | 30.8290 mL | |
| 5 mM | 0.6166 mL | 3.0829 mL | 6.1658 mL | |
| 10 mM | 0.3083 mL | 1.5414 mL | 3.0829 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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