Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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. FKBP12 PROTAC dTAG-13 (dTAG-13) is a PROTAC-based heterobifunctional degrader.
Pack Size | Availability | Price/USD | Quantity |
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5 mg | 4-5 weeks | $ 1,350.00 |
Description | 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. FKBP12 PROTAC dTAG-13 (dTAG-13) is a PROTAC-based heterobifunctional degrader. |
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. |
Synonyms | dTAG-13 |
Molecular Weight | 1049.17 |
Formula | C57H68N4O15 |
CAS No. | 2064175-41-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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FKBP12 PROTAC dTAG-13 2064175-41-1 Chromatin/Epigenetic Epigenetic Reader Domain FKBP12 PROTAC dTAG 13 dTAG-13 FKBP-12 PROTAC dTAG-13 FKBP12 PROTAC dTAG13 inhibitor inhibit