FKBP12PROTACdTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader ofFKBP12^F36Vwith expression of FKBP12F36V in-frame with a protein of interest. FKBP12PROTACdTAG-13 effectively engagesFKBP12^F36Vand CRBN, thereby selectively degradingFKBP12^F36V[1].

TAG-13 (1-1000 nM; 4 hours; 293FT^WTcells) treatment potently reduces FKBP12^F36V-Nluc levels in 293FT^WTcell, indicating the requirement of CRBN for the observed effects^[1].
Treatment of MV4;11 cells expressing BRD4(short)-FKBP12^F36Vwith 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 FKBP12^WT[1].

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].

1049.17

Solid

C₅₇H₆₈N₄O₁₅

2064175-41-1

Room temperature in continental US; may vary elsewhere.

DMSO : 180 mg/mL(171.56 mM;Need ultrasonic)

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