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PROTACBET Degrader-14 is a potent PROTAC compound designed to target BET (bromodomain and extraterminal domain) proteins. It effectively degrades all family members of BET, including BRD2, BRD3, and BRD4. The compound demonstrates significant efficacy in degrading BET proteins in the U2OS osteosarcoma cell line (BRD4 DC50 = 130 nM) and the KYSE180 esophageal squamous cell carcinoma cell line (DC50 = 40 nM). Its mechanism of degradation relies on the ubiquitin-proteasome system. Furthermore, PROTACBET Degrader-14 reduces the expression levels of BET-regulated gene products such as c-Myc, RUNX2, and KRT14, making it a valuable tool for osteosarcoma research.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | PROTACBET Degrader-14 is a potent PROTAC compound designed to target BET (bromodomain and extraterminal domain) proteins. It effectively degrades all family members of BET, including BRD2, BRD3, and BRD4. The compound demonstrates significant efficacy in degrading BET proteins in the U2OS osteosarcoma cell line (BRD4 DC50 = 130 nM) and the KYSE180 esophageal squamous cell carcinoma cell line (DC50 = 40 nM). Its mechanism of degradation relies on the ubiquitin-proteasome system. Furthermore, PROTACBET Degrader-14 reduces the expression levels of BET-regulated gene products such as c-Myc, RUNX2, and KRT14, making it a valuable tool for osteosarcoma research. |
| Targets&IC50 | BRD4:130 nM (DC50) |
| In vitro | PROTAC BET Degrader-14 (Compound 105B) exhibits a dose-dependent degradation of BRD4 in U2OS osteosarcoma cells at concentrations ranging from 0.01 to 10 μM over 24 hours. At 10 nM, it rapidly induces BRD4 degradation within 0 to 24 hours in U2OS cells, though this effect may rebound due to BRD4 resynthesis. Additionally, PROTAC BET Degrader-14 at concentrations of 0.01 nM to 1 μM for 24 hours reduces the expression levels of c-Myc and RUNX2 in U2OS osteosarcoma cells. In KYSE180 esophageal squamous cell carcinoma cells, concentrations from 0.51 nM to 10 μM lower the expression of KRT14 without degrading BRDT. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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.
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.
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