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FKBP12 PROTAC dTAG-13

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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

FKBP12 PROTAC dTAG-13

😃Good
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.
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5 mg$1,35035 days
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Product Introduction

Bioactivity
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.
AliasdTAG-13
Chemical Properties
Molecular Weight1049.17
FormulaC57H68N4O15
Cas No.2064175-41-1
Relative Density.1.260 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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