EB-TCIP
Based on 1 Customer Validation
EB-TCIP (BAK-04-212) is a proof-of-concept tool specifically designed for Ewing sarcoma research, serving as an EWSR1::FLI1 binder tagged with BCL6 and FKBP12F36V. EB-TCIP forms a ternary complex with the tagged fusion protein, specifically recruits EWSR1::FLI1 to BCL6-bound DNA loci, and induces rapid chromatin remodeling and relocalization. By mediating relocalization, EB-TCIP remodels the transcriptional machinery and activates the expression of BCL6 target genes that are originally repressed. EB-TCIP is used in studies related to novel epigenetic therapies for Ewing sarcoma.
For research use only. We do not sell to patients.
- Purity: 99.58%
- CAS No.: 3114073-95-6
- Formula: C68H86ClN9O15
- Molecular Weight:1304.91
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
EB-TCIP potently induces the formation of a ternary complex between purified FKBP12F36V and BCL6BTB, with an EC50 of 0.14 μM in cell-free assays[1].
EB-TCIP (0.1-10 μM; 1 h) dose-dependently induces the formation of a reversible ternary complex between FKBP-E::F and endogenous BCL6 in EWS502 FKBP-E::F cell lysates, with the maximum complex formation observed at concentrations of 1.0-10 μM[1].
EB-TCIP (0.001-10 μM) potently and dose-dependently induces the expression of BCL6 target transcripts (SOCS2 EC50=0.17 μM; CISH EC50=0.11 μM) and protein (SOCS2) in EWS502 FKBP-E::F cells, while reducing BCL6 protein levels. Its maximal activity occurs at a concentration of 2.5 μM, and a hook effect appears at high concentrations[1].
EB-TCIP (0.078-10 μM; 72 h) inhibits the proliferation of EWS502 FKBP-E::F cells within 72 h in a dose-dependent manner, but this activity is not mechanism-specific, as the same phenomenon is also observed in parental EWS502 cells that do not express FKBP-E::F[1].
EB-TCIP (1 μM; 1-24 h) rapidly induces BCL6 degradation in EWS502 FKBP-E::F cells (maximal effect is achieved within 1 h), and continuously and significantly upregulates the expression of SOCS2 protein, with the expression peak of SOCS2 transcripts occurring between 2 and 4 h[1].
EB-TCIP (1-2.5 μM; 4-24 h) rapidly induces genome-wide transcriptomic changes in EWS502 FKBP-E::F cells, a feature highly correlated with BCL6 knockout, including potent upregulation of BCL6 target genes such as SOCS2, CISH and CXCL11[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EWS502 FKBP-E::F and parental EWS502 cells
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Concentration:0.078-10 μM
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Incubation Time:72 h
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Result:Dose-dependently decreased proliferation of EWS502 FKBP-E::F cells over 72 h.
Showed identical antiproliferative activity in parental EWS502 cells that do not express FKBP-E::F, indicating off-mechanism cytotoxicity.
Chemical Information
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CAS No. 3114073-95-6
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Appearance Solid
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Molecular Weight 1304.91
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Formula C68H86ClN9O15
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Color White to off-white
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SMILES
COC1=C(OC)C=C([C@@H](C(N2CCCC[C@H]2C(O[C@@H](C3=CC=CC=C3OCC(NCCCCCCNC(C4CCN(C5=NC(NC(C=C6OC)=CC7=C6N(C(C(OCC(NC)=O)=C7)=O)C)=C(Cl)C=N5)CC4)=O)=O)CCC8=CC=C(OC)C(OC)=C8)=O)=O)CC)C=C1OC
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Synonyms
BAK-04-212
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (76.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (285 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.7663 mL | 3.8317 mL | 7.6634 mL | 19.1584 mL |
| 5 mM | 0.1533 mL | 0.7663 mL | 1.5327 mL | 3.8317 mL | |
| 10 mM | 0.0766 mL | 0.3832 mL | 0.7663 mL | 1.9158 mL | |
| 15 mM | 0.0511 mL | 0.2554 mL | 0.5109 mL | 1.2772 mL | |
| 20 mM | 0.0383 mL | 0.1916 mL | 0.3832 mL | 0.9579 mL | |
| 25 mM | 0.0307 mL | 0.1533 mL | 0.3065 mL | 0.7663 mL | |
| 30 mM | 0.0255 mL | 0.1277 mL | 0.2554 mL | 0.6386 mL | |
| 40 mM | 0.0192 mL | 0.0958 mL | 0.1916 mL | 0.4790 mL | |
| 50 mM | 0.0153 mL | 0.0766 mL | 0.1533 mL | 0.3832 mL | |
| 60 mM | 0.0128 mL | 0.0639 mL | 0.1277 mL | 0.3193 mL |
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