1. PROTAC
    Autophagy
    Apoptosis
    Immunology/Inflammation
    Epigenetics
  2. PROTAC
    FKBP
    Epigenetic Reader Domain
  3. FKBP12 PROTAC dTAG-13

FKBP12 PROTAC dTAG-13 (Synonyms: dTAG-13)

Cat. No.: HY-114421
Handling Instructions

FKBP12 PROTAC dTAG-13 (dTAG-13) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.

For research use only. We do not sell to patients.

FKBP12 PROTAC dTAG-13 Chemical Structure

FKBP12 PROTAC dTAG-13 Chemical Structure

CAS No. : 2064175-41-1

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products

View All PROTAC Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

FKBP12 PROTAC dTAG-13 (dTAG-13) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN[1].

IC50 & Target[1]

Cereblon

 

BRD4

 

FKBP12(F36V)

 

In Vitro

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[1].
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. 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[1].

Western Blot Analysis[1]

Cell Line: 293FTWT cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 4 hours
Result: Potently reduced FKBP12F36V-Nluc levels in 293FTWT cell.
In Vivo

Following bone marrow engraftment of MV4;11 cells expressing luc-FKBP12F36V in mice, the bioluminescent signal after vehicle or dTAG-13 administration is monitored. A significant, rapid, and durable effect on bioluminescent signal is observed four hours after dTAG-13 administration, indicating effective degradation of luc-FKBP12F36V. Twenty-eight hours following the final treatment, the recovery of cellular bioluminescence to levels comparable between vehicle and dTAG-13 treatment groups is observed[1].

Molecular Weight

1049.17

Formula

C₅₇H₆₈N₄O₁₅

CAS No.

2064175-41-1

SMILES

COC1=CC=C(CC[[email protected]](C2=C(OCC(NCCCCCCOC3=CC=CC4=C3C(N(C5CCC(NC5=O)=O)C4=O)=O)=O)C=CC=C2)OC([[email protected]@H]6CCCCN6C([[email protected]@H](CC)C7=CC(OC)=C(OC)C(OC)=C7)=O)=O)C=C1OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

FKBP12 PROTAC dTAG-13dTAG-13dTAG13dTAG 13PROTACFKBPEpigenetic Reader DomainProteolysis-targeting chimeraFK506-binding proteinBegradationCRBNFKBP12F36Vheterodimerizers rapidBRD4Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
FKBP12 PROTAC dTAG-13
Cat. No.:
HY-114421
Quantity:
MCE Japan Authorized Agent: