TP-021
Based on 1 publication(s) in Google Scholar
TP-021 (BCL6-IN-8c), a chemical probe, is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 μM in cell-free enzyme-linked immunosorbent assay.
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- Purity: 98.77%
- CAS No.: 2130878-25-8
- 화학식: C20H20ClN3O5
- 분자량:417.84
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보관: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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) TP-021
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Biological Activity
IC50: 0.10 μM (BCL6-corepressor interaction)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
0.72 μM
Compound: 8c
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Inhibition of recombinant human BCoR (112 to 753 residues) protein interaction with recombinant GAL4-fused BCL6 (5 to 129 residues) expressed in HEK293T cells measured after 20 hrs by luciferase reporter gene based mammalian two-hybrid assay
Inhibition of recombinant human BCoR (112 to 753 residues) protein interaction with recombinant GAL4-fused BCL6 (5 to 129 residues) expressed in HEK293T cells measured after 20 hrs by luciferase reporter gene based mammalian two-hybrid assay
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[PMID: 28760529] |
TP-021 (BCL6-IN-8c, Compound 8c) also exhibits good cellular PPI inhibitory activity in the submicromolar range (M2H IC50 = 0.72 μM). TP-021 (BCL6-IN-8c) does not exhibit significant cytotoxicity even at 30 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2130878-25-8
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Appearance Solid
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분자량 417.84
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화학식 C20H20ClN3O5
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Color Light yellow to yellow
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SMILES
O=C1NC2=C(CC1)C=C(C=C2)NC3=CC(OC4CCOCC4)=C(C=C3Cl)[N+]([O-])=O
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Synonyms
BCL6-IN-8c
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
용액&용해도
DMSO : ≥ 50 mg/mL (119.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.71 mg/mL (1.70 mM); Clear solution
This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 2.3933 mL | 11.9663 mL | 23.9326 mL | 59.8315 mL |
| 5 mM | 0.4787 mL | 2.3933 mL | 4.7865 mL | 11.9663 mL | |
| 10 mM | 0.2393 mL | 1.1966 mL | 2.3933 mL | 5.9832 mL | |
| 15 mM | 0.1596 mL | 0.7978 mL | 1.5955 mL | 3.9888 mL | |
| 20 mM | 0.1197 mL | 0.5983 mL | 1.1966 mL | 2.9916 mL | |
| 25 mM | 0.0957 mL | 0.4787 mL | 0.9573 mL | 2.3933 mL | |
| 30 mM | 0.0798 mL | 0.3989 mL | 0.7978 mL | 1.9944 mL | |
| 40 mM | 0.0598 mL | 0.2992 mL | 0.5983 mL | 1.4958 mL | |
| 50 mM | 0.0479 mL | 0.2393 mL | 0.4787 mL | 1.1966 mL | |
| 60 mM | 0.0399 mL | 0.1994 mL | 0.3989 mL | 0.9972 mL | |
| 80 mM | 0.0299 mL | 0.1496 mL | 0.2992 mL | 0.7479 mL | |
| 100 mM | 0.0239 mL | 0.1197 mL | 0.2393 mL | 0.5983 mL |
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