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FKBP12 PROTAC dTAG-13
Catalog No. T11291Cas No. 2064175-41-1
Alias dTAG-13
FKBP12 PROTAC dTAG-13 (dTAG-13) is a heterobifunctional degrader that targets FKBP12F36V with FKBP12F36V expressed in-frame with a protein of interest, and selectively degrades the BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to the E3 ubiquitin ligase CRBN.
FKBP12 PROTAC dTAG-13
Catalog No. T11291Alias dTAG-13Cas No. 2064175-41-1
FKBP12 PROTAC dTAG-13 (dTAG-13) is a heterobifunctional degrader that targets FKBP12F36V with FKBP12F36V expressed in-frame with a protein of interest, and selectively degrades the BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to the E3 ubiquitin ligase CRBN.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $1,350 | 35 days |
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Product Introduction
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Chemical Properties
| Description | FKBP12 PROTAC dTAG-13 (dTAG-13) is a heterobifunctional degrader that targets FKBP12F36V with FKBP12F36V expressed in-frame with a protein of interest, and selectively degrades the BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to the E3 ubiquitin ligase CRBN. |
| In vitro | dTAG-13 treatment leads to rapid and potent degradation of the BRD4 fusion chimera in the heterozygous and homozygous knock-in clones, with no effect on endogenous FKBP12WT.TAG-13 (1-1000 nM; 4 hours; 293FTWT cells) treatment potently reduces FKBP12F36V-Nluc levels in 293FTWT cell, indicating the requirement of CRBN for the observed effects. Treatment of MV4;11 cells expressing BRD4(short)-FKBP12F36V with dTAG-13 leads to robust degradation of BRD4. dTAG-13 treatment leads to rapid degradation of BRD4 within one hou. |
| In vivo | After bone marrow transplantation of mice with MV4;11 cells expressing luc-FKBP12F36V, monitoring of the bioluminescent signal reveals a significant, rapid, and lasting reduction in bioluminescence four hours after dTAG-13 administration, compared to the vehicle control, signifying effective breakdown of luc-FKBP12F36V. Moreover, 28 hours post the final dTAG-13 treatment, bioluminescence levels equalize between the dTAG-13 and vehicle groups, indicating recovery. |
| Alias | dTAG-13 |
| Molecular Weight | 1049.17 |
| Formula | C57H68N4O15 |
| Cas No. | 2064175-41-1 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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