Shopping Cart
Remove All
Your shopping cart is currently empty
TKP-5
Copy Product Info
🥰Excellent
Synonyms:
Catalog No. T218414 Copy Product Info
🥰Excellent
TKP-5 is a PROTAC protein degrader targeting BRD4. It binds to BRD2, BRD3, BRD4, and BRDT, with dissociation constants (Ka) of 150 nM, 100 nM, and 150 nM for the first three, respectively. TKP-5 inhibits thymic stromal lymphopoietin production and downregulates IL-33 mRNA expression. It is applicable for studies on tape-stripping-induced skin injury.
TKP-5
Cas No. 3076612-97-7
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
Add to Quotation
For research use only—not for human use. No sales to individuals. Use as intended only.
Resource Download
Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | TKP-5 is a PROTAC protein degrader targeting BRD4. It binds to BRD2, BRD3, BRD4, and BRDT, with dissociation constants (Ka) of 150 nM, 100 nM, and 150 nM for the first three, respectively. TKP-5 inhibits thymic stromal lymphopoietin production and downregulates IL-33 mRNA expression. It is applicable for studies on tape-stripping-induced skin injury. |
| In vitro | TKP-5 effectively degrades BRD4 in KCMH-1 cells with a DC50 of 16.78 nM when used at concentrations of 0.1-10 μM for 2-24 hours. It inhibits TSLP production in KCMH-1 cells at concentrations as low as 0.1 μM and selectively binds to the BD1 domain of BRD2, BRD3, BRD4, and BRDT at 1 μM. Through interaction between its triazole group and BRD4's Trp81, TKP-5 forms a stable ternary complex with CRBN and BRD4-BD1. Moreover, TKP-5 induces the degradation of BRD2, BRD3, and BRD4 in KCMH-1 cells at concentrations below 100 nM after 5 hours of treatment. |
| In vivo | TKP-5, administered topically at a concentration of 1% (w/w), in a single dose over 6 hours, completely inhibits IL-33 mRNA expression associated with skin damage induced by tape stripping in 8-week-old male ICR mice. |
| Molecular Weight | 833.88 |
| Formula | C44H47N7O10 |
| Cas No. | 3076612-97-7 |
| Smiles | N(C(CCCCCN1C=C(COC2=CC=C(/C=C/C(=O)C3=C(CCNC(C)=O)C=C(OC)C(OCC)=C3)C=C2)N=N1)=O)C4=C5C(C(=O)N(C5=O)C6C(=O)NC(=O)CC6)=CC=C4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Calculator
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
Preview
Related Tags: TKP-5 in vivo | TKP-5 in vitro | TKP-5 formula | TKP-5 molecular weight
Generate Quote
Catalog No.: Cas No.:
Add
| Size | Quantity | Unit Price | Amount | Operation |
|---|
Generate Quote
- TOP
Feedback
Hello! How can I help you today? 
Copyright © 2015-2026 TargetMol Chemicals Inc. All Rights Reserved.