FKBP12 PROTAC dTAG-13 (dTAG-13) 是一种基于 PROTAC 的双功能降解剂，可降解 FKBP12^F36V。FKBP12 PROTAC dTAG-13 有效地接合 FKBP12^F36V 和 CRBN，从而选择性地降解 FKBP12^F36V。

FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12 with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12 and CRBN, thereby selectively degrading FKBP12.

Solid

Cereblon FKBP12(F36V)

TAG-13 (1-1000 nM; 4 hours; 293FT cells) treatment potently reduces FKBP12-Nluc levels in 293FT cell, indicating the requirement of CRBN for the observed effects.
Treatment of MV4;11 cells expressing BRD4(short)-FKBP12 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 FKBP12. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；In solvent -80°C 6 months

[1]. Nabet B, et al. The dTAG system for immediate and target-specific protein degradation. Nat Chem Biol. 2018 May;14(5):431-441.

In Vitro: DMSO : 180 mg/mL (171.56 mM; Need ultrasonic)配制储备液