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TCIP 1
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Catalog No. T79801
TCIP 1 is a small molecule in the category of transcriptional/epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].
TCIP 1
Copy Product Info😃Good
Catalog No. T79801
TCIP 1 is a small molecule in the category of transcriptional/epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $6,055 | 3-6 months | 3-6 months | |
| 50 mg | $7,955 | 3-6 months | 3-6 months | |
| 100 mg | $10,755 | 3-6 months | 3-6 months |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | TCIP 1 is a small molecule in the category of transcriptional/epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1]. |
| In vitro | TCIP 1 enhanced the binding of BRD4 to BCL6 loci on the genome by 50%, while only reducing its binding at enhancers by 10%. This led to transcriptional elongation at pro-apoptotic target genes, significantly inhibiting diffuse large B-cell lymphoma cell lines, including chemotherapy-resistant TP53 mutant cell lines, with an EC50 of 1-10 nM [1]. The apoptosis induced by TCIP 1 could be blocked by either JQ1 (a BRD4 inhibitor) or BI3812 (a BCL6 inhibitor). TCIP 1 induced G1/S and G2/M cell cycle arrest in KARPAS422 cells. Further, TCIP 1 (10 or 100 nM; 20 h) significantly activated anti-apoptotic genes, while a 10 nM concentration for 8 h suppressed the expression of MYC and its target genes. |
| In vivo | TCIP1, administered intraperitoneally at a dosage of 10 mg/kg daily for five consecutive days, was well tolerated in wild-type C57BL/6 mice with a half-life (t 1/2) of 9.7 hours, a maximum concentration (C max) of 0.41 μM, and an area under the curve (AUC 0-last) of 1.92 μM/h [1]. |
| Molecular Weight | 1026.04 |
| Formula | C50H58Cl2N12O6S |
| Smiles | CNC(COC1=CC2=C(C(OC)=CC(NC3=NC(N4CCC(C(NCCCCCCCNC(C[C@@H]5N=C(C6=CC=C(Cl)C=C6)C7=C(SC(C)=C7C)N8C(C)=NN=C58)=O)=O)CC4)=NC=C3)=C2)N(C)C1=O)=O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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